| HepG2 |
IC50 |
= |
80.0 |
nM |
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay |
CHEMBL4311992 |
| Tubulin |
Activity |
|
|
|
Disruption of microtubule network in human HCT116 cells assessed as microtubule disorganization at 50 nM for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis |
CHEMBL4311992 |
| A549 |
IC50 |
= |
100.0 |
nM |
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay |
CHEMBL4311992 |
| HCT-116 |
IC50 |
= |
60.0 |
nM |
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay |
CHEMBL4311992 |
| Tubulin |
Activity |
|
|
|
Disruption of microtubule network in human HCT116 cells assessed as microtubule condensation at 50 nM incubated for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis |
CHEMBL4311992 |
| Tubulin |
Activity |
|
|
|
Disruption of microtubule network in human SW620 cells assessed as microtubule disorganization at 50 nM for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis |
CHEMBL4311992 |
| Tubulin |
Activity |
|
|
|
Disruption of microtubule network in human SW620 cells assessed as microtubule condensation at 50 nM incubated for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis |
CHEMBL4311992 |
| Adaptor-associated kinase |
Activity |
= |
105.0 |
% |
Inhibition of human AAK1 assessed as residual activity at 10 uM using peptide substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
108.5 |
% |
Inhibition of recombinant human ABL (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
101.0 |
% |
Inhibition of recombinant mouse ABL L782P/G784R/W785L/L786V mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
104.0 |
% |
Inhibition of recombinant human ABL H396P mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
96.5 |
% |
Inhibition of recombinant human ABL M351T mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human ABL Q252H mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
108.5 |
% |
Inhibition of recombinant human ABL T315I mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human ABL Y253F mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine kinase non-receptor protein 2 |
Activity |
= |
118.5 |
% |
Inhibition of recombinant human ACK1 (1 to 389 residues) assessed as residual activity at 10 uM using EFPIYDFLPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Activin receptor type-2A |
Activity |
= |
104.5 |
% |
Inhibition of recombinant human ACTR2 (162 to end residues) assessed as residual activity at 10 uM using casein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| ALK tyrosine kinase receptor |
Activity |
= |
112.5 |
% |
Inhibition of recombinant human ALK (1058 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEF as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase receptor R3 |
Activity |
= |
98.0 |
% |
Inhibition of recombinant human ALK1 (142 to end residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Activin receptor type-1 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human ALK2 (142 to end residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Activin receptor type-1B |
Activity |
= |
93.0 |
% |
Inhibition of recombinant human ALK4 (150 to end residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Bone morphogenetic protein receptor type-1B |
Activity |
= |
103.0 |
% |
Inhibition of recombinant human ALK6 (148 to end residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ABL2 |
Activity |
= |
115.0 |
% |
Inhibition of recombinant human ARG (38 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| AMP-activated protein kinase, alpha-1 subunit |
Activity |
= |
119.5 |
% |
Inhibition of recombinant full-length human AMPKalpha1 assessed as residual activity at 10 uM using AMARAASAAALARRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| AMP-activated protein kinase, alpha-2 subunit |
Activity |
= |
117.0 |
% |
Inhibition of recombinant full-length human AMPKalpha2 assessed as residual activity at 10 uM using AMARAASAAALARRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
121.5 |
% |
Inhibition of recombinant human ARAF Y301D/Y302D mutant (273 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
105.5 |
% |
Inhibition of recombinant mouse ARG M982V/A562 mutant (27 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase II alpha |
Activity |
= |
92.0 |
% |
Inhibition of recombinant full-length human CaMK2alpha assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase II beta |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human CaMK2beta (1 to 315 residues) assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase II gamma |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human CaMK2gamma (1 to 330 residues) assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase I delta |
Activity |
= |
107.0 |
% |
Inhibition of recombinant full-length human CaMK1delta assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase II delta |
Activity |
= |
120.5 |
% |
Inhibition of recombinant full-length human CaMK2delta assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase IV |
Activity |
= |
121.0 |
% |
Inhibition of recombinant full-length human CaMK4 assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM-kinase kinase alpha |
Activity |
= |
102.5 |
% |
Inhibition of recombinant full-length human CAMKk1 assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM-kinase kinase beta |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human CAMKk2 T85S mutant assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDC7/Cyclin B1 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant full-length human CDC7/cyclinB1 assessed as residual activity at 10 uM using Histone H1 as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase 1/cyclin B1 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant full-length human CDK1/cyclinB assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK2/Cyclin A2 |
Activity |
= |
109.5 |
% |
Inhibition of recombinant full-length human CDK2/cyclinA assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase 2/cyclin E1 |
Activity |
= |
115.0 |
% |
Inhibition of recombinant full-length human CDK2/cyclinE assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK3/Cyclin E |
Activity |
= |
113.0 |
% |
Inhibition of recombinant full-length human CDK3/cyclinE assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK4/Cyclin D3 |
Activity |
= |
91.0 |
% |
Inhibition of recombinant full-length human CDK4/cyclinD3 assessed as residual activity at 10 uM using Rb fragment as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase 5/CDK5 activator 1 |
Activity |
= |
94.0 |
% |
Inhibition of recombinant full-length human CDK5/p25 assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase 5/CDK5 activator 1 |
Activity |
= |
107.5 |
% |
Inhibition of recombinant full-length human CDK5/p35 assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK6/cyclin D3 |
Activity |
= |
98.5 |
% |
Inhibition of recombinant full-length human CDK6/cyclin D3 assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK7/Cyclin H/MNAT1 |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full length human CDK7/cyclin H/MAT1 assessed as residual activity at 10 uM using peptide substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK9/cyclin T1 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant full length human CDK9/cyclinT1 assessed as residual activity at 10 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK12/Cyclin K |
Activity |
= |
104.0 |
% |
Inhibition of recombinant full length human CDK12/cyclinK assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase 2 |
Activity |
= |
111.0 |
% |
Inhibition of human CK2 assessed as residual activity at 10 uM |
CHEMBL4311992 |
| Casein kinase II alpha |
Activity |
= |
88.0 |
% |
Inhibition of recombinant full length human CK2alpha1 assessed as residual activity at 10 uM using RRRDDDSDDD as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase II alpha |
Activity |
= |
89.5 |
% |
Inhibition of recombinant full length human CK2alpha2 assessed as residual activity at 10 uM using RRRDDDSDDD as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 35 |
Activity |
= |
65.5 |
% |
Inhibition of recombinant full length human CLIK1 assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificty protein kinase CLK1 |
Activity |
= |
108.0 |
% |
Inhibition of recombinant human CLK1 (130 to end residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity protein kinase CLK2 |
Activity |
= |
131.5 |
% |
Inhibition of recombinant human CLK2 (138 to end residues) assessed as residual activity at 10 uM using YRRAAVPPSPSLSRHSSPHQS(p)EDEEE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity protein kinase CLK3 |
Activity |
= |
116.0 |
% |
Inhibition of recombinant full-length human CLK3 assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity protein kinase CLK4 |
Activity |
= |
98.5 |
% |
Inhibition of recombinant human CLK4 (128 to end residues) assessed as residual activity at 10 uM using YRRAAVPPSPSLSRHSSPHQS(p)EDEEE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Stem cell growth factor receptor |
Activity |
= |
99.5 |
% |
Inhibition of recombinant human c-Kit (544 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Stem cell growth factor receptor |
Activity |
= |
93.0 |
% |
Inhibition of recombinant human c-Kit D816V mutant (544 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Stem cell growth factor receptor |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human c-Kit D816H mutant (544 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Stem cell growth factor receptor |
Activity |
= |
95.5 |
% |
Inhibition of recombinant human c-Kit V560G mutant (544 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Stem cell growth factor receptor |
Activity |
= |
90.0 |
% |
Inhibition of recombinant human c-Kit V654A mutant (544 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Citron Rho-interacting kinase |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human CRIK assessed as residual activity at 10 uM using KKLRRTLSVA as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase CSK |
Activity |
= |
98.0 |
% |
Inhibition of full-length recombinant human CSK assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase RAF |
Activity |
= |
96.5 |
% |
Inhibition of recombinant human c-RAF Y340D/Y341D mutant (360 to end residues) assessed as residual activity at 10 uM using inactive MEK1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase SRC |
Activity |
= |
130.5 |
% |
Inhibition of recombinant full-length human SRC assessed as residual activity at 10 uM using Cdc2 peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Death-associated protein kinase 1 |
Activity |
= |
114.5 |
% |
Inhibition of recombinant human DAPK1 (1 to 296 residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Death-associated protein kinase 2 |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full-length human DAPK2 assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase DCLK2 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant human DCAMKL2 (376 to end residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 5 |
Activity |
= |
99.0 |
% |
Inhibition of recombinant human EphA5 (655 to 956 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 7 |
Activity |
= |
98.5 |
% |
Inhibition of recombinant human EphA7 (613 to 909 residues) assessed as residual activity at 10 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 8 |
Activity |
= |
97.0 |
% |
Inhibition of recombinant human EphA8 (615 to 911 residues) assessed as residual activity at 10 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
93.5 |
% |
Inhibition of recombinant human EphB2 A848S/ K918E mutant (560 to end residues) assessed as residual activity at 10 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-B receptor 1 |
Activity |
= |
104.0 |
% |
Inhibition of recombinant human EphB1 (564 to end residues) assessed as residual activity at 10 uM using KVEKIGEGTYGVVYK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-B receptor 3 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant human EphB3 (599 to 920 residues) assessed as residual activity at 10 uM using poly (Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-B receptor 4 |
Activity |
= |
101.5 |
% |
Inhibition of recombinant human EphB4 (561 to end residues) assessed as residual activity at 10 uM using poly (Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Receptor protein-tyrosine kinase erbB-2 |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human ErbB2 G778D mutant (676 to end residues) assessed as residual activity at 10 uM using poly (Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Receptor protein-tyrosine kinase erbB-4 |
Activity |
= |
103.0 |
% |
Inhibition of recombinant human ErbB4 (706 to 991 residues) assessed as residual activity at 10 uM using poly (Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Focal adhesion kinase 1 |
Activity |
= |
103.5 |
% |
Inhibition of recombinant human FAK (411 to 686 residues) assessed as residual activity at 10 uM using EEEEYEEEEEEYYIIEEEEEEYEEEEEEYYEEEEEEKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase FER |
Activity |
= |
107.5 |
% |
Inhibition of recombinant human FER (541 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase FES |
Activity |
= |
100.5 |
% |
Inhibition of recombinant human FES (2 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 1 |
Activity |
= |
108.0 |
% |
Inhibition of recombinant human FGFR1 (456 to 765 residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 1 |
Activity |
= |
95.5 |
% |
Inhibition of recombinant human FGFR1 V561M mutant (456 to 765 residues) assessed as residual activity at 10 uM using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 2 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human FGFR2 (456 to 770 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 2 |
Activity |
= |
88.0 |
% |
Inhibition of recombinant human FGFR2 N549H mutant (456 to 770 residues) assessed as residual activity at 10 uM using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 3 |
Activity |
= |
94.5 |
% |
Inhibition of recombinant human FGFR3 (447 to 761 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Fibroblast growth factor receptor 4 |
Activity |
= |
100.5 |
% |
Inhibition of recombinant human FGFR4 (442 to 755 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase FGR |
Activity |
= |
94.5 |
% |
Inhibition of recombinant human FGR (2 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Vascular endothelial growth factor receptor 1 |
Activity |
= |
97.5 |
% |
Inhibition of recombinant human Flt1 (783 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Homeodomain-interacting protein kinase 2 |
Activity |
= |
104.0 |
% |
Inhibition of recombinant human HIPK2 I471N mutant (165 to 564 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Homeodomain-interacting protein kinase 3 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human HIPK3 (161 to 562 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Homeodomain-interacting protein kinase 4 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant full-length human HIPK4 assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase kinase 1 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human HPK1 (1 to 346 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Eukaryotic translation initiation factor 2-alpha kinase 1 |
Activity |
= |
102.5 |
% |
Inhibition of recombinant human HRI (140 to end residues) assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase ICK |
Activity |
= |
114.5 |
% |
Inhibition of recombinant human ICK (1 to 312 residues) assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Insulin-like growth factor I receptor |
Activity |
= |
81.0 |
% |
Inhibition of recombinant human IGF1R (959 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Insulin-like growth factor I receptor |
Activity |
= |
90.5 |
% |
Inhibition of recombinant human activated IGF1R (959 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Inhibitor of nuclear factor kappa B kinase alpha subunit |
Activity |
= |
88.5 |
% |
Inhibition of recombinant full-length human IKKalpha (959 to end residues) assessed as residual activity at 10 uM using peptide substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Inhibitor of nuclear factor kappa B kinase beta subunit |
Activity |
= |
101.5 |
% |
Inhibition of recombinant full-length human IKKbeta assessed as residual activity at 10 uM using peptide substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Inhibitor of nuclear factor kappa B kinase epsilon subunit |
Activity |
= |
98.5 |
% |
Inhibition of recombinant full-length human IKKepsilon assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Insulin receptor |
Activity |
= |
116.5 |
% |
Inhibition of recombinant human IR (1005 to 1310 residues) assessed as residual activity at 10 uM using KKSRGDYMTMQIG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Insulin receptor |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human activated IR (1005 to 1310 residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase/endoribonuclease IRE1 |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human IRE1 (465 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Insulin receptor-related protein |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human IRR (943 to 1266 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Interleukin-1 receptor-associated kinase 1 |
Activity |
= |
101.5 |
% |
Inhibition of recombinant human IRAK1 (194 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ITK/TSK |
Activity |
= |
63.0 |
% |
Inhibition of recombinant human ITK (352 to 617 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase JAK1 |
Activity |
= |
97.5 |
% |
Inhibition of recombinant human JAK1 (866 to end residues) assessed as residual activity at 10 uM using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase JAK2 |
Activity |
= |
115.0 |
% |
Inhibition of recombinant human JAK2 (808 to end residues) assessed as residual activity at 10 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase kinase 5 |
Activity |
= |
130.0 |
% |
Inhibition of recombinant full-length human MAP4K5 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
124.0 |
% |
Inhibition of recombinant human MAPKAPK2 A399G mutant (46 to end residues) assessed as residual activity at 10 uM using KKLNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase-activated protein kinase 3 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human MAPKAPK3 (2 to end residues) assessed as residual activity at 10 uM using KKLNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity mitogen-activated protein kinase kinase 1 |
Activity |
= |
100.0 |
% |
Inhibition of recombinant full-length human MEK1 assessed as residual activity at 10 uM using unactive MAPK2 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity mitogen-activated protein kinase kinase 2 |
Activity |
= |
109.0 |
% |
Inhibition of recombinant full-length human MEK2 assessed as residual activity at 10 uM using MBP as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
111.5 |
% |
Inhibition of recombinant human MARK1 T20S mutant (2 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase c-TAK1 |
Activity |
= |
90.0 |
% |
Inhibition of recombinant full-length human MARK3 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP/microtubule affinity-regulating kinase 4 |
Activity |
= |
123.0 |
% |
Inhibition of recombinant full-length human MARK4 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 2 |
Activity |
= |
104.5 |
% |
Inhibition of recombinant full-length human MEKK2 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 3 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant full-length human MEKK3 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Maternal embryonic leucine zipper kinase |
Activity |
= |
113.5 |
% |
Inhibition of recombinant human MELK (1 to 340 residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human Mer H628Q/R794A mutant (557 to 882 residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
80.0 |
% |
Inhibition of recombinant human MET A1209G/V1290L mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
107.5 |
% |
Inhibition of recombinant human MET A1209G/V1290L/D1246H mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
112.0 |
% |
Inhibition of recombinant human MET A1209G/V1290L/D1246N mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
105.0 |
% |
Inhibition of recombinant human MET A1209G/V1290L/M1268T mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
110.5 |
% |
Inhibition of recombinant human MET A1209G/V1290L/Y1248C mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
102.5 |
% |
Inhibition of recombinant human MET A1209G/V1290L/Y1248D mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Hepatocyte growth factor receptor |
Activity |
= |
99.0 |
% |
Inhibition of recombinant human MET A1209G/V1290L/Y1248H mutant (974 to end residues) assessed as residual activity at 10 uM using KKKGQEEEYVFIE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Misshapen-like kinase 1 |
Activity |
= |
94.0 |
% |
Inhibition of recombinant human MINK (1 to 310 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| FKBP12A/mTOR |
Activity |
= |
96.5 |
% |
Inhibition of recombinant full-length human mTOR/FKBP12 assessed as residual activity at 10 uM measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Muscle, skeletal receptor tyrosine protein kinase |
Activity |
= |
113.5 |
% |
Inhibition of recombinant human MuSK (530 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| myosin light chain kinase 2 |
Activity |
= |
98.0 |
% |
Inhibition of recombinant full-length human MYLK2 assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Myosin-IIIB |
Activity |
= |
111.0 |
% |
Inhibition of recombinant full-length human MYO3B (1 to 326 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 38-like |
Activity |
= |
108.0 |
% |
Inhibition of recombinant human NDR2 (83 to end residues) assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Nek1 |
Activity |
= |
114.0 |
% |
Inhibition of recombinant human NEK1 (1 to 505 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase NEK2 |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full-length human NEK2 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Nek4 |
Activity |
= |
103.5 |
% |
Inhibition of recombinant full-length human NEK4 P225A mutant assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Nek3 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant full-length human NEK3 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase NEK6 |
Activity |
= |
108.5 |
% |
Inhibition of recombinant human NEK6 (2 to end residues) assessed as residual activity at 10 uM using FLAKSFGSPNRAYKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase NEK7 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human NEK7 (2 to end residues) assessed as residual activity at 10 uM using FLAKSFGSPNRAYKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase NEK9 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human NEK9 (1 to 324 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase NIM1 |
Activity |
= |
106.0 |
% |
Inhibition of recombinant full-length human NIM1 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Nek11 |
Activity |
= |
101.5 |
% |
Inhibition of recombinant full-length human NEK11 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine protein kinase NLK |
Activity |
= |
93.5 |
% |
Inhibition of recombinant human NLK (121 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| NUAK family SNF1-like kinase 2 |
Activity |
= |
114.5 |
% |
Inhibition of recombinant full-length human NUAK2 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
105.0 |
% |
Inhibition of recombinant human p70S6K T412E mutant (1 to 421 residues) assessed as residual activity at 10 uM using KKRNRTLTV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PAK 1 |
Activity |
= |
96.0 |
% |
Inhibition of recombinant human PAK1 (150 to end residues) assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
119.0 |
% |
Inhibition of recombinant human PAK2 L150F/P225T/A339 deletion/V383I mutant (3 to end residues) assessed as residual activity at 10 uM using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PAK 4 |
Activity |
= |
106.0 |
% |
Inhibition of recombinant human PAK4 (295 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
105.0 |
% |
Inhibition of recombinant full-length human PKBalpha S478G mutant assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase AKT2 |
Activity |
= |
113.5 |
% |
Inhibition of recombinant full-length human PKBbeta S474D mutant (120 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase AKT3 |
Activity |
= |
91.0 |
% |
Inhibition of recombinant full-length human PKBgamma S472D mutant (117 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C alpha |
Activity |
= |
88.5 |
% |
Inhibition of recombinant full-length human PKCalpha assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C beta |
Activity |
= |
96.0 |
% |
Inhibition of recombinant human PKCbeta1 (2 to end residues) assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C beta |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human PKCbeta2 (2 to end residues) assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C gamma |
Activity |
= |
108.5 |
% |
Inhibition of recombinant full-length human PKCgamma assessed as residual activity at 10 uM using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C delta |
Activity |
= |
111.0 |
% |
Inhibition of recombinant human PKCdelta (2 to end residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C epsilon |
Activity |
= |
95.0 |
% |
Inhibition of recombinant human PKCepsilon (2 to end residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C eta |
Activity |
= |
98.5 |
% |
Inhibition of recombinant human PKCeta V108L/G109R/L392Q mutant (2 to end residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C iota |
Activity |
= |
105.0 |
% |
Inhibition of recombinant full-length human PKCiota assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C mu |
Activity |
= |
103.0 |
% |
Inhibition of recombinant full-length human PKCmu R135A mutant assessed as residual activity at 10 uM using KKLNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C theta |
Activity |
= |
103.0 |
% |
Inhibition of recombinant full-length human PKCtheta assessed as residual activity at 10 uM using histone H1as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C zeta |
Activity |
= |
99.5 |
% |
Inhibition of recombinant human PKCzeta (2 to end residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase D2 |
Activity |
= |
120.0 |
% |
Inhibition of recombinant full-length human PKD2 assessed as residual activity at 10 uM using KKLNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase C nu |
Activity |
= |
105.5 |
% |
Inhibition of recombinant full-length human PKD3 assessed as residual activity at 10 uM using KKLRRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| cGMP-dependent protein kinase 1 beta |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human PKG1alpha assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| cGMP-dependent protein kinase 1 beta |
Activity |
= |
111.5 |
% |
Inhibition of recombinant full-length human PKG1beta assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Interferon-induced, double-stranded RNA-activated protein kinase |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human PKR (252 to end residues) assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PLK1 |
Activity |
= |
111.5 |
% |
Inhibition of recombinant full-length human Plk1 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor TYRO3 |
Activity |
= |
125.5 |
% |
Inhibition of human RSE (451 to end residues) using KVEKIGEGTYGVVYK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 1 |
Activity |
= |
111.5 |
% |
Inhibition of recombinant full-length human Rsk1 assessed as residual activity at 10 uM using KKKNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 1 |
Activity |
= |
104.0 |
% |
Inhibition of recombinant full-length rat Rsk1 S637N/G697A mutant assessed as residual activity at 10 uM using KKKNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 3 |
Activity |
= |
100.0 |
% |
Inhibition of human Rsk2 (2 to end residues) using KKKNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 2 |
Activity |
= |
114.0 |
% |
Inhibition of recombinant full-length human Rsk3 assessed as residual activity at 10 uM using KKKNRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 6 |
Activity |
= |
98.5 |
% |
Inhibition of recombinant full-length human Rsk4 assessed as residual activity at 10 uM using LRRASLG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase p38 alpha |
Activity |
= |
109.0 |
% |
Inhibition of recombinant full-length human SAPK2a assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase p38 alpha |
Activity |
= |
100.5 |
% |
Inhibition of recombinant full-length human SAPK2a T106M mutant assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase p38 beta |
Activity |
= |
100.5 |
% |
Inhibition of recombinant full-length human SAPK2b assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase p38 gamma |
Activity |
= |
96.5 |
% |
Inhibition of recombinant full-length human SAPK3 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase p38 delta |
Activity |
= |
96.5 |
% |
Inhibition of recombinant full-length human SAPK4 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SBK1 |
Activity |
= |
107.0 |
% |
Inhibition of recombinant full-length human SBK1 assessed as residual activity at 10 uM using KKLRRTLSVA as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Sgk1 |
Activity |
= |
136.0 |
% |
Inhibition of recombinant human SGK S422D mutant (60 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Sgk2 |
Activity |
= |
111.5 |
% |
Inhibition of recombinant human SGK2 S416D mutant (54 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Sgk3 |
Activity |
= |
102.0 |
% |
Inhibition of human SGK3 (119 to end residues) using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SIK1 |
Activity |
= |
104.0 |
% |
Inhibition of human SIK (1 to 281 residues) using AMARAASAAALARRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SIK2 |
Activity |
= |
97.0 |
% |
Inhibition of human SIK2 (1 to 276 residues) using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SIK3 |
Activity |
= |
119.0 |
% |
Inhibition of human SIK3 (1 to 307 residues) using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 2 |
Activity |
= |
95.5 |
% |
Inhibition of human SLK (1 to 373 residues) using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PLK2 |
Activity |
= |
105.5 |
% |
Inhibition of human Snk (65 to 409 residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| TGF-beta receptor type I |
Activity |
= |
98.0 |
% |
Inhibition of human TGFBR1 T204D mutant (200 to end residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| TGF-beta receptor type II |
Activity |
= |
71.0 |
% |
Inhibition of human TGFBR2 (188 to end residues) using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase TIE-2 |
Activity |
= |
75.5 |
% |
Inhibition of human Tie2 Q939H/Q940H mutant (771 to end residues) using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase TIE-2 |
Activity |
= |
102.5 |
% |
Inhibition of human Tie2 Q939H/Q940H/R849W mutant (771 to end residues) using EFPIYDFLPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase TIE-2 |
Activity |
= |
114.5 |
% |
Inhibition of human Tie2 Q939H/Q940H/Y897S mutant (771 to end residues) using EFPIYDFLPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase tousled-like 1 |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full-length human TLK1 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase tousled-like 2 |
Activity |
= |
119.0 |
% |
Inhibition of human TLK2 (387 to end residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| TRAF2- and NCK-interacting kinase |
Activity |
= |
108.0 |
% |
Inhibition of human TNIK (1 to 367 residues) using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tribbles homolog 2 |
Activity |
= |
90.5 |
% |
Inhibition of recombinant full-length human TRB2 assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Nerve growth factor receptor Trk-A |
Activity |
= |
92.0 |
% |
Inhibition of human TrkA (440 to end residues) using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Neurotrophic tyrosine kinase receptor type 2 |
Activity |
= |
125.5 |
% |
Inhibition of human TrkB (455 to end residues) using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| NT-3 growth factor receptor |
Activity |
= |
109.5 |
% |
Inhibition of human TrkC (510 to end residues) using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Testis-specific serine/threonine-protein kinase 1 |
Activity |
= |
110.5 |
% |
Inhibition of recombinant full-length human TSSK1 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Testis-specific serine/threonine-protein kinase 2 |
Activity |
= |
117.0 |
% |
Inhibition of recombinant full-length human TSSK2 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Testis-specific serine/threonine-protein kinase 3 |
Activity |
= |
124.5 |
% |
Inhibition of recombinant full-length human TSSK3 assessed as residual activity at 10 uM using AMARAASAAALARRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Testis-specific serine/threonine-protein kinase 4 |
Activity |
= |
138.5 |
% |
Inhibition of recombinant full-length human TSSK4 assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tau-tubulin kinase 1 |
Activity |
= |
102.0 |
% |
Inhibition of human TTBK1 (1 to 479 residues) using Casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tau-tubulin kinase 2 |
Activity |
= |
103.5 |
% |
Inhibition of human TTBK2 (1 to 331 residues) using Casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity protein kinase TTK |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human TTK S389A mutant assessed as residual activity at 10 uM using MBP as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase TXK |
Activity |
= |
84.0 |
% |
Inhibition of human Txk (256 to end residues) using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
109.0 |
% |
Inhibition of recombinant full-length human PI3K p120gamma R459Q mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human PI3K p110delta/p85alpha N253S mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length mouse PI3K p110alpha/p85alpha assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
103.5 |
% |
Inhibition of recombinant full-length mouse PI3K p110alpha/p65alpha (1 to 571 residues) assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
99.0 |
% |
Inhibition of recombinant full-length mouse PI3K p110alpha/p85alpha E545K mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
99.0 |
% |
Inhibition of recombinant full-length mouse PI3K p110alpha/p85alpha H1047R mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full-length mouse PI3K p110beta/p85beta R123L mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
103.5 |
% |
Inhibition of recombinant full-length mouse PI3K p110beta/p85alpha R123L mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| PI3K p110 delta/p85 alpha |
Activity |
= |
100.0 |
% |
Inhibition of recombinant full-length mouse PI3K p110delta/p85alpha assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
95.0 |
% |
Inhibition of recombinant full-length mouse PI3K p110alpha/p85alpha E542K mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| NUAK family SNF1-like kinase 1 |
Activity |
= |
107.5 |
% |
Inhibition of recombinant human ARK5 (2 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 5 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human ASK1 (649 to 946 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
103.0 |
% |
Inhibition of recombinant full-length human AURKA I31F mutant assessed as residual activity at 10 uM using LRRASLG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Aurora-B |
Activity |
= |
143.0 |
% |
Inhibition of recombinant full-length human AURKB assessed as residual activity at 10 uM using AKRRRLSSLRA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Aurora-C |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human AURKC (35 to end residues) assessed as residual activity at 10 uM using AKRRRLSSLRA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor UFO |
Activity |
= |
107.0 |
% |
Inhibition of recombinant human AXL Q764R mutant (473 to end residues) assessed as residual activity at 10 uM using KKSRGDYMTMQIG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| BMP-2-inducible protein kinase |
Activity |
= |
83.0 |
% |
Inhibition of recombinant human BIKepsilon assessed as residual activity at 10 uM using peptide substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase BLK |
Activity |
= |
115.0 |
% |
Inhibition of full-length recombinant human BLK M287V mutant assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Bone morphogenetic protein receptor type-2 |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human BMPR2 (172 to 734 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase BMX |
Activity |
= |
132.0 |
% |
Inhibition of full-length recombinant human BMX assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase BRK |
Activity |
= |
100.5 |
% |
Inhibition of full-length recombinant human BRK assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| BR serine/threonine-protein kinase 1 |
Activity |
= |
140.0 |
% |
Inhibition of recombinant human BrSK1 (2 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
123.0 |
% |
Inhibition of recombinant human BrSK2 S251I mutant (2 to end residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase BTK |
Activity |
= |
85.0 |
% |
Inhibition of full-length recombinant human BTK assessed as residual activity at 10 uM using KVEKIGEGTYGVVYK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase BTK |
Activity |
= |
98.0 |
% |
Inhibition of full-length recombinant human BTK R28H mutant assessed as residual activity at 10 uM using LSNLYHQGKFLQTFCGSPLYRRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase B-raf |
Activity |
= |
121.5 |
% |
Inhibition of recombinant human BRAF (416 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase B-raf |
Activity |
= |
107.5 |
% |
Inhibition of recombinant human BRAF V599E mutant (416 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase I alpha |
Activity |
= |
109.0 |
% |
Inhibition of recombinant human CaMK1 (2 to end residues) assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Calcium/calmodulin-dependent protein kinase type 1B |
Activity |
= |
107.0 |
% |
Inhibition of recombinant full-length human CaMK1beta assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CaM kinase I gamma |
Activity |
= |
126.0 |
% |
Inhibition of human CaMK1gamma |
CHEMBL4311992 |
| Cyclin-dependent kinase 13/Cyclin-K |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full length human CDK13/cyclinK assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase 14/Cyclin-Y |
Activity |
= |
96.5 |
% |
Inhibition of human CDK14/cyclinY assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Cyclin-Y/Cyclin-dependent kinase 16 |
Activity |
= |
123.0 |
% |
Inhibition of recombinant full length human CDK16/cyclinY assessed as residual activity at 10 uM using PKSPKARKKL as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK17/Cyclin-Y |
Activity |
= |
102.5 |
% |
Inhibition of human CDK17/cyclinY assessed as residual activity at 10 uM using PKSPKARKKL as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| CDK18/Cyclin Y |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full length human cyclinY/CDK18 T166M mutant assessed as residual activity at 10 uM using YRRAAVPPSPSLS as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase-like 1 |
Activity |
= |
121.5 |
% |
Inhibition of recombinant human CDKL1 (1 to 303 residues) assessed as residual activity at 10 uM using RRRFRPASPLRGP as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase-like 2 |
Activity |
= |
131.0 |
% |
Inhibition of human CDKL2 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Cyclin-dependent kinase-like 3 |
Activity |
= |
126.5 |
% |
Inhibition of recombinant human full-length CDKL3 (1 to 303 residues) assessed as residual activity at 10 uM using RRRFRPASPLRGP as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Cyclin-dependent kinase-like 4 |
Activity |
= |
116.5 |
% |
Inhibition of human CDKL4 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Transient receptor potential cation channel subfamily M member 7 |
Activity |
= |
108.5 |
% |
Inhibition of recombinant human CHAK1 (1180 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Chk1 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant full length human CHK1 assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Histone-lysine N-methyltransferase EZH2 |
Inhibition |
= |
-10.0 |
% |
Inhibition of EZH2 (unknown origin) at 1 uM relative to control |
CHEMBL4311992 |
| Histone-lysine N-methyltransferase EZH2 |
Inhibition |
= |
-9.0 |
% |
Inhibition of EZH2 (unknown origin) at 10 uM relative to control |
CHEMBL4311992 |
| SW-620 |
IC50 |
= |
60.0 |
nM |
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| CT26 |
IC50 |
= |
45.5 |
nM |
Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| SW480 |
IC50 |
= |
64.5 |
nM |
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| DLD-1 |
IC50 |
= |
135.5 |
nM |
Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| HCT-15 |
IC50 |
= |
61.0 |
nM |
Antiproliferative activity against human HCT15 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| HT-29 |
IC50 |
= |
71.0 |
nM |
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| MDA-MB-231 |
IC50 |
= |
200.5 |
nM |
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| A549 |
IC50 |
= |
98.0 |
nM |
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Anticancer activity against human HCT116 cells assessed as reduction in cell viability by MTT assay |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Anticancer activity against human SW620 cells assessed as reduction in cell viability by MTT assay |
CHEMBL4311992 |
| HCT-116 |
Inhibition |
= |
100.0 |
% |
Inhibition of colony formation in human HCT116 cells at 50 nM after 14 days by crystal violet staining-based microscopic analysis |
CHEMBL4311992 |
| SW-620 |
Inhibition |
= |
100.0 |
% |
Inhibition of colony formation in human SW620 cells at 50 nM after 14 days by crystal violet staining-based microscopic analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase after 24 hrs by propidium iodide-staining based flow cytometry |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of cell cycle arrest in human SW620 cells assessed as accumulation at G2/M phase after 24 hrs by propidium iodide-staining based flow cytometry |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Cell cycle arrest in human HCT116 cells assessed as up regulation of CyclinB1 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Cell cycle arrest in human HCT116 cells assessed as up regulation of CDK1 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Cell cycle arrest in human HCT116 cells assessed as up regulation of cdc25 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Cell cycle arrest in human HCT116 cells assessed as increase in dephosphorylation of CDK1 up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Cell cycle arrest in human SW620 cells assessed as up regulation of CyclinB1 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Cell cycle arrest in human SW620 cells assessed as up regulation of CDK1 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Cell cycle arrest in human SW620 cells assessed as up regulation of cdc25 expression up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Cell cycle arrest in human SW620 cells assessed as increase in dephosphorylation of CDK1 up to 150 nM after 24 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells assessed as increase in Bax expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells assessed as increase in cleaved caspase9 expression measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells assessed as increase in cleaved caspase3 expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells assessed as increase in cleaved PARP expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Induction of apoptosis in human HCT116 cells assessed as decrease in Bcl2 expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells assessed as increase in Bax expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells assessed as increase in cleaved caspase9 expression measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells assessed as increase in cleaved caspase3 expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells assessed as increase in cleaved PARP expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Induction of apoptosis in human SW620 cells assessed as decrease in Bcl2 expression up to 200 nM measured after 48 hrs by Western blot analysis |
CHEMBL4311992 |
| HCT-116 |
TGI |
= |
39.9 |
% |
Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 40 mg/kg, po administered once daily for 4 weeks measured post-last dose relative to control |
CHEMBL4311992 |
| HCT-116 |
TGI |
= |
71.6 |
% |
Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 80 mg/kg, po administered once daily for 4 weeks measured post-last dose relative to control |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as reduction in tumor weight at 40 mg/kg, po administered once daily for 4 weeks measured every 3 days during compound dosing |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as reduction in tumor weight at 80 mg/kg, po administered once daily for 4 weeks measured every 3 days during compound dosing |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as change in body weight at 40 mg/kg, po administered once daily for 4 weeks measured every 3 days during compound dosing |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as change in body weight at 80 mg/kg, po administered once daily for 4 weeks measured every 3 days during compound dosing |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Cardiotoxicity in nude BALB/c mouse at 80 mg/kg, po administered once daily for 4 weeks measured post-last dose by hematoxylin and eosin staining-based assay |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Hepatotoxicity in nude BALB/c mouse at 80 mg/kg, po administered once daily for 4 weeks measured post-last dose by hematoxylin and eosin staining-based assay |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in Balb/c mouse spleen at 80 mg/kg after 4 weeks by hematoxylin and eosin staining-based assay |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in Balb/c mouse lung at 80 mg/kg after 4 weeks by hematoxylin and eosin staining-based assay |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Renal toxicity in nude BALB/c mouse at 80 mg/kg, po administered once daily for 4 weeks measured post-last dose by hematoxylin and eosin staining-based assay |
CHEMBL4311992 |
| Serine/threonine-protein kinase Chk2 |
Activity |
= |
105.0 |
% |
Inhibition of recombinant human CHK2 (5 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Chk2 |
Activity |
= |
103.0 |
% |
Inhibition of recombinant human CHK2 I157T mutant (5 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase Chk2 |
Activity |
= |
103.0 |
% |
Inhibition of recombinant human CHK2 R145W mutant (5 to end residues) assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I epsilon |
Activity |
= |
100.0 |
% |
Inhibition of human CK1epsilon assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I gamma 1 |
Activity |
= |
94.5 |
% |
Inhibition of recombinant human CK1gamma1 (25 to 355 residues) assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I gamma 2 |
Activity |
= |
104.5 |
% |
Inhibition of recombinant human CK1gamma2 (18 to end residues) assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I isoform gamma-3 |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human CK1gamma3 K91E/R174G/E302D mutant (1 to 330 residues) assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I delta |
Activity |
= |
103.0 |
% |
Inhibition of recombinant human CK1delta (1 to 294 residues) assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Casein kinase I |
Activity |
= |
106.5 |
% |
Inhibition of CK1 (unknown origin) assessed as residual activity at 10 uM |
CHEMBL4311992 |
| Serine/threonine-protein kinase DCLK3 |
Activity |
= |
109.5 |
% |
Inhibition of recombinant human DCAMKL3 (345 to end residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
113.5 |
% |
Inhibition of recombinant human DDR1 V833L mutant (492 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Discoidin domain-containing receptor 2 |
Activity |
= |
97.0 |
% |
Inhibition of recombinant human DDR2 S642A mutant (467 to end residues) assessed as residual activity at 10 uM using KKSRGDYMTMQIG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Myotonin-protein kinase |
Activity |
= |
103.5 |
% |
Inhibition of recombinant human DMPK (1 to 549 residues) assessed as residual activity at 10 uM using KKSRGDYMTMQIG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 17A |
Activity |
= |
91.5 |
% |
Inhibition of recombinant full-length human DRAK1 assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 17B |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full-length human DRAK2 assessed as residual activity at 10 uM using KKRPQRRYSNVF as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual-specificity tyrosine-phosphorylation regulated kinase 1A |
Activity |
= |
100.5 |
% |
Inhibition of recombinant full-length human DYRK1A assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B |
Activity |
= |
100.0 |
% |
Inhibition of recombinant full-length human DYRK1B assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual-specificity tyrosine-phosphorylation regulated kinase 2 |
Activity |
= |
113.0 |
% |
Inhibition of recombinant full-length human DYRK2 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual-specificity tyrosine-phosphorylation regulated kinase 3 |
Activity |
= |
121.5 |
% |
Inhibition of recombinant full-length human DYRK3 assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase EEF2K |
Activity |
= |
104.0 |
% |
Inhibition of recombinant human EEF2K H23R mutant (2 to end residues) assessed as residual activity at 10 uM using RKKFGESEKTKTKEFL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Epidermal growth factor receptor erbB1 |
Activity |
= |
114.0 |
% |
Inhibition of recombinant human EGFR (696 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Epidermal growth factor receptor erbB1 |
Activity |
= |
104.0 |
% |
Inhibition of recombinant human EGFR L858R mutant (696 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Epidermal growth factor receptor erbB1 |
Activity |
= |
98.5 |
% |
Inhibition of recombinant human EGFR L861Q mutant (696 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Epidermal growth factor receptor erbB1 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human EGFR T790M mutant (696 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Epidermal growth factor receptor erbB1 |
Activity |
= |
96.5 |
% |
Inhibition of recombinant human EGFR T790M/L858R mutant (696 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 1 |
Activity |
= |
102.5 |
% |
Inhibition of recombinant human EphA1 (568 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEF as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 2 |
Activity |
= |
91.0 |
% |
Inhibition of recombinant human EphA2 (596 to 900 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 3 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human EphA3 (578 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ephrin type-A receptor 4 |
Activity |
= |
100.0 |
% |
Inhibition of recombinant human EphA4 (601 to 892 residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor FLT3 |
Activity |
= |
85.5 |
% |
Inhibition of recombinant human Flt3 D835Y mutant (564 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor FLT3 |
Activity |
= |
130.5 |
% |
Inhibition of recombinant human Flt3 (564 to end residues) assessed as residual activity at 10 uM using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
103.5 |
% |
Inhibition of recombinant human Flt4 V1128L/H1146R mutant (800 to end residues) assessed as residual activity at 10 uM using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Macrophage colony stimulating factor receptor |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human FMS (538 to end residues) assessed as residual activity at 10 uM using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Macrophage colony stimulating factor receptor |
Activity |
= |
94.5 |
% |
Inhibition of recombinant human FMS Y969C mutant (538 to end residues) assessed as residual activity at 10 uM using EEEEYEEEEEEYYIIEEEEEEYEEEEEEYYEEEEEEKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase FYN |
Activity |
= |
98.0 |
% |
Inhibition of recombinant full-length human FYN assessed as residual activity at 10 uM using Cdc2 peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase kinase 2 |
Activity |
= |
100.5 |
% |
Inhibition of recombinant human GCK assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Eukaryotic translation initiation factor 2-alpha kinase 4 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant full-length human GCN2 E556G mutant assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Rhodopsin kinase |
Activity |
= |
90.5 |
% |
Inhibition of recombinant full-length human GRK1 assessed as residual activity at 10 uM using KKKKERLLDDRHDSGLDSMKDEE as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| G-protein coupled receptor kinase 2 |
Activity |
= |
102.5 |
% |
Inhibition of recombinant full-length human GRK2 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Beta-adrenergic receptor kinase 2 |
Activity |
= |
100.5 |
% |
Inhibition of recombinant full-length human GRK3 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Beta-adrenergic receptor kinase 2 |
Activity |
= |
105.0 |
% |
Inhibition of recombinant full-length human GRK5 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| G protein-coupled receptor kinase 6 |
Activity |
= |
104.5 |
% |
Inhibition of recombinant full-length human GRK6 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| G protein-coupled receptor kinase 7 |
Activity |
= |
102.0 |
% |
Inhibition of recombinant full-length human GRK7 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Glycogen synthase kinase-3 alpha |
Activity |
= |
102.0 |
% |
Inhibition of recombinant human GSK3alpha (2 to end residues) assessed as residual activity at 10 uM using phospho GS2 peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Glycogen synthase kinase-3 beta |
Activity |
= |
112.5 |
% |
Inhibition of recombinant human GSK3beta H350L mutant (2 to end residues) assessed as residual activity at 10 uM using phospho GS2 peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase haspin |
Activity |
= |
89.0 |
% |
Inhibition of recombinant human haspin (471 to end residues) assessed as residual activity at 10 uM using RARTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase HCK |
Activity |
= |
106.0 |
% |
Inhibition of recombinant human HCK (230 to 497 residues) assessed as residual activity at 10 uM using Cdc2 peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase HCK |
Activity |
= |
115.0 |
% |
Inhibition of recombinant human activated HCK (230 to 497 residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Homeodomain-interacting protein kinase 1 |
Activity |
= |
100.0 |
% |
Inhibition of recombinant human activated HIPK1 (158 to 555 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase JAK3 |
Activity |
= |
90.0 |
% |
Inhibition of recombinant human JAK3 (781 to end residues) assessed as residual activity at 10 uM using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| c-Jun N-terminal kinase 1 |
Activity |
= |
96.0 |
% |
Inhibition of recombinant full-length human JNK1alpha1 assessed as residual activity at 10 uM using ATF2 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
103.0 |
% |
Inhibition of recombinant full-length human JNK2alpha2 S51N mutant assessed as residual activity at 10 uM using ATF2 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| c-Jun N-terminal kinase 3 |
Activity |
= |
141.5 |
% |
Inhibition of recombinant full-length human JNK3 assessed as residual activity at 10 uM using peptide substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Vascular endothelial growth factor receptor 2 |
Activity |
= |
107.0 |
% |
Inhibition of recombinant human KDR (790 to end residues) assessed as residual activity at 10 uM using myelin basic protein substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase LCK |
Activity |
= |
84.5 |
% |
Inhibition of recombinant full-length human Lck assessed as residual activity at 10 uM using KVEKIGEGTYGVV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase LCK |
Activity |
= |
102.0 |
% |
Inhibition of recombinant full-length human activated Lck assessed as residual activity at 10 uM using KVEKIGEGTYGVVYK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| LIM domain kinase 1 |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human LIMK1 (285 to 638 residues) assessed as residual activity at 10 uM using cofilin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| LIM domain kinase 2 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant human LIMK2 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 11 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant full-length human LKB1 assessed as residual activity at 10 uM using LSNLYHQGKFLQTFCGSPLYRRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 10 |
Activity |
= |
91.5 |
% |
Inhibition of recombinant human LOK (1 to 348 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase Lyn |
Activity |
= |
119.0 |
% |
Inhibition of recombinant full-length human Lyn assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Leucine-rich repeat serine/threonine-protein kinase 2 |
Activity |
= |
100.0 |
% |
Inhibition of recombinant human LRRK2 (970 to end residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Leukocyte tyrosine kinase receptor |
Activity |
= |
101.5 |
% |
Inhibition of recombinant human LTK (450 to end residues) assessed as residual activity at 10 uM using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MAK |
Activity |
= |
106.5 |
% |
Inhibition of recombinant full-length human MAK assessed as residual activity at 10 uM using RRRFRPASPLRGPPK as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase ERK2 |
Activity |
= |
97.5 |
% |
Inhibition of recombinant full-length human MAPK1 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP kinase ERK2 |
Activity |
= |
103.5 |
% |
Inhibition of human MAPK2 assessed as residual activity at 10 uM |
CHEMBL4311992 |
| MAP kinase ERK2 |
Activity |
= |
97.5 |
% |
Inhibition of mouse MAPK2 assessed as residual activity at 10 uM |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase kinase 3 |
Activity |
= |
103.5 |
% |
Inhibition of recombinant human MAP4K3 (1 to 291 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase kinase 4 |
Activity |
= |
114.0 |
% |
Inhibition of recombinant human MAP4K4 (1 to 328 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity mitogen-activated protein kinase kinase 3 |
Activity |
= |
100.5 |
% |
Inhibition of human MKK3 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Dual specificity mitogen-activated protein kinase kinase 4 |
Activity |
= |
133.0 |
% |
Inhibition of recombinant human MKK4 (34 to end residues) assessed as residual activity at 10 uM using unactive JNK1a1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Dual specificity mitogen-activated protein kinase kinase 6 |
Activity |
= |
114.0 |
% |
Inhibition of recombinant human MKK6 (4 to end residues) assessed as residual activity at 10 uM using unactive SAPK2a as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Myosin light chain kinase, smooth muscle |
Activity |
= |
94.0 |
% |
Inhibition of recombinant human MLCK (1425 to 1771 residues) assessed as residual activity at 10 uM using calmodulin as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 9 |
Activity |
= |
104.5 |
% |
Inhibition of recombinant human MLK1 (134 to 414 residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 10 |
Activity |
= |
91.0 |
% |
Inhibition of recombinant human MLK2 (1 to 449 residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 11 |
Activity |
= |
104.5 |
% |
Inhibition of human MLK3 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| MAP kinase signal-integrating kinase 2 |
Activity |
= |
88.0 |
% |
Inhibition of recombinant full-length human Mnk2 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAPK/MAK/MRK overlapping kinase |
Activity |
= |
104.5 |
% |
Inhibition of recombinant human MOK (1 to 343 residues) assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MRCK-A |
Activity |
= |
110.0 |
% |
Inhibition of recombinant human MRCKalpha (1 to 473 residues) assessed as residual activity at 10 uM using KKRNRTLTV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MRCK beta |
Activity |
= |
112.5 |
% |
Inhibition of recombinant human MRCKbeta (1 to 473 residues) assessed as residual activity at 10 uM using KKRNRTLTV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MRCK gamma |
Activity |
= |
122.0 |
% |
Inhibition of recombinant human MRCKgamma assessed as residual activity at 10 uM using KKRNRTLTV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 5 |
Activity |
= |
111.5 |
% |
Inhibition of recombinant human MSK1 (2 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Ribosomal protein S6 kinase alpha 4 |
Activity |
= |
120.5 |
% |
Inhibition of recombinant human MSK2 (2 to end residues) assessed as residual activity at 10 uM using GRPRTSSFAEGKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SRPK3 |
Activity |
= |
130.5 |
% |
Inhibition of recombinant full-length human MSSK1 assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MST1 |
Activity |
= |
122.0 |
% |
Inhibition of recombinant full-length human MST1 assessed as residual activity at 10 uM using KKSRGDYMTMQIG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MST2 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant full-length human MST2 (2 to end residues) assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 24 |
Activity |
= |
110.0 |
% |
Inhibition of recombinant human MST3 (1 to 304 residues) assessed as residual activity at 10 uM using ERMRPRKRQGSVRRRV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase MST4 |
Activity |
= |
132.0 |
% |
Inhibition of recombinant human MST4 (4 to 304 residues) assessed as residual activity at 10 uM using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase mTOR |
Activity |
= |
78.5 |
% |
Inhibition of recombinant full-length human mTOR assessed as residual activity at 10 uM measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PAK 3 |
Activity |
= |
134.0 |
% |
Inhibition of recombinant full-length human PAK3 assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PAK7 |
Activity |
= |
110.5 |
% |
Inhibition of recombinant human PAK5 (425 to end residues) assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PAK6 |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human PAK6 (382 to end residues) assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| MAP/microtubule affinity-regulating kinase 2 |
Activity |
= |
95.5 |
% |
Inhibition of recombinant full-length human PAR1Balpha assessed as residual activity at 10 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| PAS domain-containing serine/threonine-protein kinase |
Activity |
= |
100.0 |
% |
Inhibition of recombinant human PASK (995 to end residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Eukaryotic translation initiation factor 2-alpha kinase 3 |
Activity |
= |
116.5 |
% |
Inhibition of recombinant human PEK (536 to end residues) assessed as residual activity at 10 uM using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Platelet-derived growth factor receptor alpha |
Activity |
= |
97.5 |
% |
Inhibition of recombinant human PDGFRalpha (550 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Platelet-derived growth factor receptor alpha |
Activity |
= |
101.0 |
% |
Inhibition of recombinant human PDGFRalpha D842V mutant (550 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Platelet-derived growth factor receptor alpha |
Activity |
= |
106.5 |
% |
Inhibition of recombinant human PDGFRalpha V561D mutant (550 to end residues) assessed as residual activity at 10 uM using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Platelet-derived growth factor receptor beta |
Activity |
= |
117.0 |
% |
Inhibition of recombinant human PDGFRbeta (557 to end residues) assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Pyruvate dehydrogenase kinase isoform 2 |
Activity |
= |
128.5 |
% |
Inhibition of human PDHK2 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Pyruvate dehydrogenase kinase isoform 4 |
Activity |
= |
95.0 |
% |
Inhibition of recombinant full-length human PDHK4 assessed as residual activity at 10 uM using KKKYHGHSMSDPGVSYRT as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| 3-phosphoinositide dependent protein kinase-1 |
Activity |
= |
91.0 |
% |
Inhibition of recombinant human PDK1 (52 to end residues) assessed as residual activity at 10 uM using PDKtide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Phosphorylase kinase gamma subunit 1 |
Activity |
= |
104.0 |
% |
Inhibition of recombinant full-length human PhKgamma1 assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Phosphorylase kinase gamma subunit 2 |
Activity |
= |
92.0 |
% |
Inhibition of recombinant human PhKgamma2 F290L mutant (1 to 301 residues) assessed as residual activity at 10 uM using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PIM1 |
Activity |
= |
105.5 |
% |
Inhibition of recombinant full-length human Pim1 assessed as residual activity at 10 uM using KKRNRTLTV as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PIM2 |
Activity |
= |
103.5 |
% |
Inhibition of recombinant human Pim2 (2 to end residues) assessed as residual activity at 10 uM using RSRHSSYPAGT as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PIM3 |
Activity |
= |
107.0 |
% |
Inhibition of recombinant human Pim3 (2 to end residues) assessed as residual activity at 10 uM using RSRHSSYPAGT as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| cAMP-dependent protein kinase alpha-catalytic subunit |
Activity |
= |
91.0 |
% |
Inhibition of recombinant full-length human PKA assessed as residual activity at 10 uM using Kemptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| cAMP-dependent protein kinase beta-1 catalytic subunit |
Activity |
= |
98.5 |
% |
Inhibition of recombinant full-length human PKAC beta assessed as residual activity at 10 uM using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PLK3 |
Activity |
= |
99.5 |
% |
Inhibition of recombinant human Plk3 (19 to 301 residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
98.5 |
% |
Inhibition of recombinant human Plk4 S34T mutant (1 to 273 residues) assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
125.0 |
% |
Inhibition of recombinant human PRAK R291E mutant assessed as residual activity at 10 uM using KKLRRTLSVA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| cGMP-dependent protein kinase 2 |
Activity |
= |
98.0 |
% |
Inhibition of recombinant full-length human PRKG2 assessed as residual activity at 10 uM using KKLRRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase N1 |
Activity |
= |
98.5 |
% |
Inhibition of human PRK1 V901I mutant (498 to end residues) using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein kinase N2 |
Activity |
= |
115.5 |
% |
Inhibition of human PRK2 (501 to end residues) using AKRRRLSSLRA as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PRKX |
Activity |
= |
113.0 |
% |
Inhibition of recombinant full-length human PrKX assessed as residual activity at 10 uM using RRRLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase PRP4 homolog |
Activity |
= |
93.0 |
% |
Inhibition of human PRP4 (663 to end residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase FRK |
Activity |
= |
101.5 |
% |
Inhibition of human PTK5 (218 to end residues) using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Protein tyrosine kinase 2 beta |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full-length human Pyk2 assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor RET |
Activity |
= |
100.0 |
% |
Inhibition of human Ret (658 to end residues) using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor RET |
Activity |
= |
105.5 |
% |
Inhibition of human Ret V804L mutant (658 to end residues) using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase receptor RET |
Activity |
= |
105.5 |
% |
Inhibition of human Ret V804M mutant (658 to end residues) using KKKVSRSGLYRSPSMPENLNRPR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Receptor-interacting serine/threonine-protein kinase 1 |
Activity |
= |
92.0 |
% |
Inhibition of human RIPK1 (8 to 322 residues) using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase RIPK2 |
Activity |
= |
105.5 |
% |
Inhibition of human RIPK2 (1 to 299 residues) using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Rho-associated protein kinase 1 |
Activity |
= |
109.5 |
% |
Inhibition of human ROCK1 (17 to 535 residues) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Rho-associated protein kinase 2 |
Activity |
= |
105.0 |
% |
Inhibition of human ROCK2 (11 to 552 residues) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Rho-associated protein kinase 2 |
Activity |
= |
109.5 |
% |
Inhibition of rat ROCK2 A9P/S341Q/A342H/S343P mutant (2 to 543 residues) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Macrophage-stimulating protein receptor |
Activity |
= |
110.0 |
% |
Inhibition of human Ron (983 to end residues) using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
102.5 |
% |
Inhibition of human Ros V2262A mutant (1883 to end residues) using KKKSPGEYVNIEFG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| SNF-related serine/threonine-protein kinase |
Activity |
= |
111.0 |
% |
Inhibition of human SNRK E97G/P116A mutant (65 to 409 residues) using KKLRRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase SRC |
Activity |
= |
123.5 |
% |
Inhibition of human Src (1 to 530 residues) using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase SRC |
Activity |
= |
122.0 |
% |
Inhibition of recombinant full-length human Src T341M mutant assessed as residual activity at 10 uM using GGEEEEYFELVKKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase Srms |
Activity |
= |
108.5 |
% |
Inhibition of human SRMS assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SRPK1 |
Activity |
= |
101.0 |
% |
Inhibition of human SRPK1 (2 to end residues) using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase SRPK2 |
Activity |
= |
105.5 |
% |
Inhibition of human SRPK2 (46 to end residues) using RSRSRSRSRSRSRSR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 16 |
Activity |
= |
101.5 |
% |
Inhibition of human STK16 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 25 |
Activity |
= |
106.5 |
% |
Inhibition of human STK25 (1 to 308 residues) using RLGRDKYKTLRQIRQ as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 32A |
Activity |
= |
100.5 |
% |
Inhibition of recombinant full-length human STK32A assessed as residual activity at 10 uM using casein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 32B |
Activity |
= |
98.0 |
% |
Inhibition of recombinant full-length human STK32B assessed as residual activity at 10 uM using casein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 32C |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full-length human STK32C assessed as residual activity at 10 uM using casein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase 33 |
Activity |
= |
86.5 |
% |
Inhibition of recombinant full-length human STK33 assessed as residual activity at 10 uM using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase SYK |
Activity |
= |
123.0 |
% |
Inhibition of recombinant full-length human Syk assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Transcription initiation factor TFIID subunit 1-like |
Activity |
= |
108.0 |
% |
Inhibition of human TAF1L (1428 to end residues) using RRRFRPASPLRGPPK as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mitogen-activated protein kinase kinase kinase 7 |
Activity |
= |
98.5 |
% |
Inhibition of human TAK1 (1 to 303 residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase TAO1 |
Activity |
= |
93.5 |
% |
Inhibition of human TAO1 (1 to 327 residues) using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase TAO2 |
Activity |
= |
104.0 |
% |
Inhibition of human TAO2 (1 to 320 residues) using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase TAO3 |
Activity |
= |
97.0 |
% |
Inhibition of human TAO3 (1 to 411 residues) using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase TBK1 |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human TBK1 assessed as residual activity at 10 uM using KRRRALS(p)VASLPGL as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
96.5 |
% |
Inhibition of human activated Tec F514V mutant (174 to end residues) using EFPIYDFLPAKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase TYK2 |
Activity |
= |
95.5 |
% |
Inhibition of human TYK2 (875 to end residues) using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase ULK1 |
Activity |
= |
104.0 |
% |
Inhibition of human ULK1 (1 to 314 residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase ULK2 |
Activity |
= |
103.0 |
% |
Inhibition of human ULK2 (1 to 306 residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase ULK3 |
Activity |
= |
101.5 |
% |
Inhibition of recombinant full-length human ULK3 assessed as residual activity at 10 uM using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase VRK1 |
Activity |
= |
92.5 |
% |
Inhibition of human VRK1 assessed as residual activity at 10 uM by radiometric method |
CHEMBL4311992 |
| Serine/threonine-protein kinase VRK2 |
Activity |
= |
102.5 |
% |
Inhibition of human VRK2 (1 to 336 residues) using casein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase WEE1 |
Activity |
= |
84.5 |
% |
Inhibition of human Wee1 (214 to end residues) using LSNLYHQGKFLQTFCGSPLYRRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Wee1-like protein kinase 2 |
Activity |
= |
95.0 |
% |
Inhibition of recombinant full-length human WEE1b assessed as residual activity at 10 uM using LSNLYHQGKFLQTFCGSPLYRRR as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase WNK1 |
Activity |
= |
103.5 |
% |
Inhibition of human WNK1 (1 to 491 residues) using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase WNK2 |
Activity |
= |
109.5 |
% |
Inhibition of human WNK2 (166 to 489 residues) using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase WNK3 |
Activity |
= |
135.5 |
% |
Inhibition of human WNK3 (1 to 434 residues) using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine/threonine-protein kinase WNK4 |
Activity |
= |
98.5 |
% |
Inhibition of human WNK4 using myelin basic protein as substrate measured after 120 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase YES |
Activity |
= |
79.0 |
% |
Inhibition of recombinant full-length human Yes assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Mixed lineage kinase 7 |
Activity |
= |
97.0 |
% |
Inhibition of recombinant full-length human ZAK assessed as residual activity at 10 uM using MBP as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Tyrosine-protein kinase ZAP-70 |
Activity |
= |
95.5 |
% |
Inhibition of recombinant full-length human ZAP70 assessed as residual activity at 10 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Death-associated protein kinase 3 |
Activity |
= |
109.5 |
% |
Inhibition of human ZIPK (1 to 290 residues) using KKLNRTLSFAEPG as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method |
CHEMBL4311992 |
| Serine-protein kinase ATM |
Activity |
= |
95.5 |
% |
Inhibition of recombinant full-length human ATM assessed as residual activity at 10 uM using GST-cMyc-p53 as substrate measured after 40 mins by ELISA |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
106.0 |
% |
Inhibition of recombinant full-length human ATRIP/ATR M211T mutant assessed as residual activity at 10 uM using GST-cMyc-p53 as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| DNA-dependent protein kinase |
Activity |
= |
99.0 |
% |
Inhibition of recombinant full-length human DNA-PK assessed as residual activity at 10 uM using GST-cMyc-p53 as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| PI3K p110 beta/p85 alpha |
Activity |
= |
103.5 |
% |
Inhibition of recombinant full-length human PI3K p110beta/p85alpha assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| PI3-kinase p110-alpha/p85-alpha |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human PI3K p110alpha/p85alpha assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| PI3-kinase p110-alpha/p85-alpha |
Activity |
= |
97.5 |
% |
Inhibition of recombinant full-length human PI3K p110alpha/p85alpha E542K mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| PI3-kinase p110-alpha/p85-alpha |
Activity |
= |
101.0 |
% |
Inhibition of recombinant full-length human PI3K p110alpha/p85alpha H1047R mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| PI3-kinase p110-alpha/p85-alpha |
Activity |
= |
93.5 |
% |
Inhibition of recombinant full-length human PI3K p110alpha/p85alpha E545K mutant assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by fluorescence assay |
CHEMBL4311992 |
| Unchecked |
Activity |
= |
93.0 |
% |
Inhibition of recombinant full-length human PI3K p110alpha/p65alpha (1 to 571 residues) assessed as residual activity at 10 uM using phosphatidylinositol-4, 5-bisphosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha |
Activity |
= |
112.5 |
% |
Inhibition of recombinant human PI3KC2alpha (299 to end residues) assessed as residual activity at 10 uM using phosphatidylinositol as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma |
Activity |
= |
100.5 |
% |
Inhibition of recombinant human PI3KC2gamma (468 to 1203 residues) assessed as residual activity at 10 uM using phosphatidylinositol as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Phosphatidylinositol-5-phosphate 4-kinase type-2 alpha |
Activity |
= |
108.0 |
% |
Inhibition of recombinant full-length human PIP4K2alpha assessed as residual activity at 10 uM using phosphatidylinositol 5-phosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| PLC-PRF-5 |
IC50 |
= |
286.0 |
nM |
Antiproliferative activity against human PLC/PRF/5 cells assessed as reduction in cell viability after 72 hrs by MTT assay |
CHEMBL4311992 |
| HCT-116 |
Activity |
|
|
|
Anticancer activity against human HCT116 cells assessed as reduction in cell viability by MTT assay |
CHEMBL4311992 |
| SW-620 |
Activity |
|
|
|
Anticancer activity against human SW620 cells assessed as reduction in cell viability by MTT assay |
CHEMBL4311992 |
| Tubulin |
Inhibition |
|
|
% |
Inhibition of porcine brain tubulin polymerization at 0.05 to 30 uM by fluorescence assay |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
95.9 |
% |
Induction of apoptosis in human HCT116 cells assessed as viable cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.5%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
1.54 |
% |
Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.418%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
17.1 |
% |
Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 3.87%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
0.846 |
% |
Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.16%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
42.6 |
% |
Induction of apoptosis in human HCT116 cells assessed as viable cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.5%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
3.57 |
% |
Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.418%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
46.2 |
% |
Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 3.87%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
7.59 |
% |
Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.16%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
39.0 |
% |
Induction of apoptosis in human HCT116 cells assessed as viable cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.5%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
5.35 |
% |
Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.418%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
42.6 |
% |
Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 3.87%) |
CHEMBL4311992 |
| HCT-116 |
Activity |
= |
5.57 |
% |
Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.16%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
61.8 |
% |
Induction of apoptosis in human SW620 cells assessed as viable cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.7%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
1.22 |
% |
Induction of apoptosis in human SW620 cells assessed as early apoptotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.773%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
4.23 |
% |
Induction of apoptosis in human SW620 cells assessed as late apoptotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.8%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
2.71 |
% |
Induction of apoptosis in human SW620 cells assessed as necrotic cells at 25 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2.71%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
83.4 |
% |
Induction of apoptosis in human SW620 cells assessed as viable cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.7%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
1.01 |
% |
Induction of apoptosis in human SW620 cells assessed as early apoptotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.773%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
9.24 |
% |
Induction of apoptosis in human SW620 cells assessed as late apoptotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.8%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
6.3 |
% |
Induction of apoptosis in human SW620 cells assessed as necrotic cells at 50 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2.71%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
66.0 |
% |
Induction of apoptosis in human SW620 cells assessed as viable cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 94.7%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
3.55 |
% |
Induction of apoptosis in human SW620 cells assessed as early apoptotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.773%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
23.1 |
% |
Induction of apoptosis in human SW620 cells assessed as late apoptotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 1.8%) |
CHEMBL4311992 |
| SW-620 |
Activity |
= |
6.55 |
% |
Induction of apoptosis in human SW620 cells assessed as necrotic cells at 100 nM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 2.71%) |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in platelet level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in RBC level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in albumin level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in globulin level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in total protein level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in ALT level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in AST level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in uric acid level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in cholesterol level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in glucose level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
| Phosphatidylinositol-4-phosphate 5-kinase type-1 alpha |
Activity |
= |
100.0 |
% |
Inhibition of recombinant full-length human PIP5K1alpha assessed as residual activity at 10 uM using phosphatidylinositol 4-phosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| Phosphatidylinositol-4-phosphate 5-kinase type-1 gamma |
Activity |
= |
99.5 |
% |
Inhibition of recombinant full-length human PIP5K1gamma assessed as residual activity at 10 uM using phosphatidylinositol 4-phosphate as substrate measured after 40 mins by HTRF assay |
CHEMBL4311992 |
| ADMET |
Activity |
|
|
|
Toxicity in nude BALB/c mouse assessed as change in WBC level at 40 to 80 mg/kg, po once daily for 4 weeks measured post-last dose |
CHEMBL4311992 |
