| Phosphatidylinositol 4-kinase, PI4K |
IC50 |
= |
218000.0 |
nM |
Inhibitory activity (IC50) against human phosphatidylinositol 4-kinase at the ATP binding site |
CHEMBL1124860 |
| Phosphatidylinositol 4-kinase, PI4K |
Ki |
= |
150200.0 |
nM |
Binding affinity (Ki) against human phosphatidylinositol 4-kinase |
CHEMBL1124860 |
| GABA-A receptor; anion channel |
Inhibition |
= |
57.0 |
% |
The percent inhibition of [3H]diazepam binding to the benzodiazepine receptor of rat brain elicited by 100 uM of compound |
CHEMBL1124455 |
| Unchecked |
IC50 |
= |
300000.0 |
nM |
Inhibition of p34cdc2/cyclin B |
CHEMBL1145498 |
| HeLa |
Activity |
= |
5.0 |
mM |
Cell cycle arrest in human HeLa cells assessed as accumulation at S phase |
CHEMBL1145498 |
| Mitogen-activated protein kinase kinase kinase 5 |
Inhibition |
> |
30.0 |
% |
Inhibition of ASK1 assessed as phosphorylated fluorescent peptide at 10 uM by mobility shift assay |
CHEMBL1641590 |
| Ribosomal protein S6 kinase alpha 3 |
Ki |
= |
5011.87 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: RPS6KA3 |
CHEMBL1201862 |
| Protein kinase C delta |
Ki |
= |
12589.25 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKCD |
CHEMBL1201862 |
| Serine/threonine-protein kinase c-TAK1 |
Ki |
= |
5011.87 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: MARK3 |
CHEMBL1201862 |
| Serine/threonine-protein kinase Chk1 |
Ki |
= |
12589.25 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CHEK1 |
CHEMBL1201862 |
| Serine/threonine-protein kinase Aurora-A |
Ki |
= |
3981.07 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: STK6 |
CHEMBL1201862 |
| Serine/threonine-protein kinase Chk2 |
Ki |
= |
3981.07 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CHEK2 |
CHEMBL1201862 |
| MAP/microtubule affinity-regulating kinase 2 |
Ki |
= |
7943.28 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: MARK2 |
CHEMBL1201862 |
| cAMP-dependent protein kinase alpha-catalytic subunit |
Ki |
= |
15848.93 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKACA |
CHEMBL1201862 |
| 3-phosphoinositide dependent protein kinase-1 |
Ki |
= |
7943.28 |
nM |
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PDPK1 |
CHEMBL1201862 |
| Cyclin-dependent kinase 2/cyclin E1 |
Ki |
= |
1096.48 |
nM |
Inhibition of human recombinant CDK2/CycE using HHASPRK as substrate by ESI-MS analysis |
CHEMBL2029332 |
| Tyrosine-protein kinase ZAP-70 |
Ki |
< |
10000.0 |
nM |
Inhibition of human recombinant ZAP70 using EEEEYEEEE as substrate by ESI-MS analysis |
CHEMBL2029332 |
| Protein tyrosine kinase 2 beta |
Ki |
< |
10000.0 |
nM |
Inhibition of human recombinant PYK2 by ESI-MS analysis |
CHEMBL2029332 |
| No relevant target |
LogD7.4 |
|
0.95 |
|
ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake flask method described in J. Biomol. Screen. 2011, 16, 348-355. Experimental range -1.5 to 4.5 |
CHEMBL3301361 |
| AMP-activated protein kinase, alpha-2 subunit |
Thermal melting change |
= |
-0.6 |
degrees C |
Delta TM value showing the stabilisation of AMPKA2 produced by compound binding |
CHEMBL1145498 |
| CaM kinase I delta |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of CAMK1D produced by compound binding |
CHEMBL1145498 |
| CaM kinase I gamma |
Thermal melting change |
= |
-0.1 |
degrees C |
Delta TM value showing the stabilisation of CAMK1G produced by compound binding |
CHEMBL1145498 |
| CaM kinase II alpha |
Thermal melting change |
= |
1.7 |
degrees C |
Delta TM value showing the stabilisation of CAMK2A produced by compound binding |
CHEMBL1145498 |
| CaM kinase II beta |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of CAMK2B produced by compound binding |
CHEMBL1145498 |
| CaM kinase II delta |
Thermal melting change |
= |
-0.2 |
degrees C |
Delta TM value showing the stabilisation of CAMK2D produced by compound binding |
CHEMBL1145498 |
| CaM kinase II gamma |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of CAMK2G produced by compound binding |
CHEMBL1145498 |
| CaM kinase IV |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of CAMK4 produced by compound binding |
CHEMBL1145498 |
| CaM-kinase kinase beta |
Thermal melting change |
= |
1.0 |
degrees C |
Delta TM value showing the stabilisation of CAMKK2 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase 2 |
Thermal melting change |
= |
0.3 |
degrees C |
Delta TM value showing the stabilisation of CDK2 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase 6 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of CDK6 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase-like 1 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of CDKL1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase Chk2 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of CHEK2 produced by compound binding |
CHEMBL1145498 |
| Dual specificty protein kinase CLK1 |
Thermal melting change |
= |
1.3 |
degrees C |
Delta TM value showing the stabilisation of CLK1 produced by compound binding |
CHEMBL1145498 |
| Dual specificity protein kinase CLK2 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of CLK2 produced by compound binding |
CHEMBL1145498 |
| Dual specificity protein kinase CLK3 |
Thermal melting change |
= |
0.4 |
degrees C |
Delta TM value showing the stabilisation of CLK3 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I gamma 1 |
Thermal melting change |
= |
-0.1 |
degrees C |
Delta TM value showing the stabilisation of CK1G1 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I gamma 2 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of CK1G2 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I isoform gamma-3 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of CK1G3 produced by compound binding |
CHEMBL1145498 |
| Death-associated protein kinase 3 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of DAPK3 produced by compound binding |
CHEMBL1145498 |
| Myotonin-protein kinase |
Thermal melting change |
= |
0.8 |
degrees C |
Delta TM value showing the stabilisation of DMPK1 produced by compound binding |
CHEMBL1145498 |
| Glycogen synthase kinase-3 beta |
Thermal melting change |
= |
0.7 |
degrees C |
Delta TM value showing the stabilisation of GSK3B produced by compound binding |
CHEMBL1145498 |
| Tyrosine-protein kinase JAK1 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of JAK1~B produced by compound binding |
CHEMBL1145498 |
| Dual specificity mitogen-activated protein kinase kinase 2 |
Thermal melting change |
= |
-0.2 |
degrees C |
Delta TM value showing the stabilisation of MEK2 produced by compound binding |
CHEMBL1145498 |
| Dual specificity mitogen-activated protein kinase kinase 6 |
Thermal melting change |
= |
0.2 |
degrees C |
Delta TM value showing the stabilisation of MAP2K6 produced by compound binding |
CHEMBL1145498 |
| Mitogen-activated protein kinase kinase kinase 5 |
Thermal melting change |
= |
2.8 |
degrees C |
Delta TM value showing the stabilisation of ASK1 produced by compound binding |
CHEMBL1145498 |
| MAP kinase p38 beta |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of p38beta produced by compound binding |
CHEMBL1145498 |
| MAP kinase ERK1 |
Thermal melting change |
= |
0.4 |
degrees C |
Delta TM value showing the stabilisation of ERK1 produced by compound binding |
CHEMBL1145498 |
| Mitogen-activated protein kinase 6 |
Thermal melting change |
= |
-0.1 |
degrees C |
Delta TM value showing the stabilisation of ERK3 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase MST4 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of MST4(1) produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase NEK2 |
Thermal melting change |
= |
0.8 |
degrees C |
Delta TM value showing the stabilisation of NEK2 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase NEK6 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of NEK6 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase OSR1 |
Thermal melting change |
= |
1.1 |
degrees C |
Delta TM value showing the stabilisation of OSR1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK 4 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of PAK4 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK7 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of PAK5 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK6 |
Thermal melting change |
= |
-0.3 |
degrees C |
Delta TM value showing the stabilisation of PAK6 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PCTAIRE-1 |
Thermal melting change |
= |
-0.3 |
degrees C |
Delta TM value showing the stabilisation of PCTK1 produced by compound binding |
CHEMBL1145498 |
| 3-phosphoinositide dependent protein kinase-1 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of PDK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM1 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of PIM1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM2 |
Thermal melting change |
= |
0.3 |
degrees C |
Delta TM value showing the stabilisation of PIM2 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM3 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of PIM3 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PLK1 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of PLK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PLK4 |
Thermal melting change |
= |
1.3 |
degrees C |
Delta TM value showing the stabilisation of PLK4 produced by compound binding |
CHEMBL1145498 |
| cAMP-dependent protein kinase alpha-catalytic subunit |
Thermal melting change |
= |
0.7 |
degrees C |
Delta TM value showing the stabilisation of PRKACA produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase RIO2 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of RIOK2 produced by compound binding |
CHEMBL1145498 |
| Ribosomal protein S6 kinase alpha 3 |
Thermal melting change |
= |
0.6 |
degrees C |
Delta TM value showing the stabilisation of RSK2a produced by compound binding |
CHEMBL1145498 |
| Ribosomal protein S6 kinase alpha 3 |
Thermal melting change |
= |
0.8 |
degrees C |
Delta TM value showing the stabilisation of RSK2b produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 2 |
Thermal melting change |
= |
0.8 |
degrees C |
Delta TM value showing the stabilisation of SLK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 10 |
Thermal melting change |
= |
-0.4 |
degrees C |
Delta TM value showing the stabilisation of LOK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 16 |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of MPSK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 17A |
Thermal melting change |
= |
1.5 |
degrees C |
Delta TM value showing the stabilisation of DRAK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 38 |
Thermal melting change |
= |
0.3 |
degrees C |
Delta TM value showing the stabilisation of NDR1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase MST4 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of MST4 (2) produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase MST1 |
Thermal melting change |
= |
1.1 |
degrees C |
Delta TM value showing the stabilisation of MST1 produced by compound binding |
CHEMBL1145498 |
| TRAF2- and NCK-interacting kinase |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of TNIK produced by compound binding |
CHEMBL1145498 |
| PDZ-binding kinase |
Thermal melting change |
= |
0.5 |
degrees C |
Delta TM value showing the stabilisation of PBK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase VRK1 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of VRK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase VRK2 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of VRK2 produced by compound binding |
CHEMBL1145498 |
| Inactive serine/threonine-protein kinase VRK3 |
Thermal melting change |
= |
-1.0 |
degrees C |
Delta TM value showing the stabilisation of VRK3 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 25 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of YSK1 produced by compound binding |
CHEMBL1145498 |
| Unchecked |
MOTILITY REDUCTION/CYTOTOXICITY |
= |
0.0 |
% |
GSK PKIS2: Screen against O. lienalis microfilariae, single point, at 3.1uM to assess reduction in motility. Compounds were also tested for cytotoxicity against Rhesus Monkey LLCMK2 cells. A score was assigned as follows: Score 3 = Good activity, 100 % motility reduction; Score 2 = Marginal/moderate activity, 50-99% motility reduction; Score 1 = Inactive, <50% motility reduction; Score 0 = Cytotoxic. |
CHEMBL3988181 |
| Heat shock protein HSP90 |
IC50 |
= |
1500000.0 |
nM |
Inhibition of HSP90 (unknown origin) by confocal fluorescence-based biochemical assay |
CHEMBL4665682 |
| Leucine-rich repeat serine/threonine-protein kinase 2 |
IC50 |
= |
3355.0 |
nM |
Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti-phospho-LRRKtide antibody addition and measured after 30 mins by TR-FRET based Lanthascreen kinase activity assay |
CHEMBL5038598 |
| Leucine-rich repeat serine/threonine-protein kinase 2 |
Ki |
= |
1425.0 |
nM |
Binding affinity to human GST tagged truncated LRRK2 G2019S mutant incubated for 2 hrs by TR-FRET based Lanthascreen kinase activity assay |
CHEMBL5038598 |
