| Adenosine kinase |
Ki |
= |
30.0 |
nM |
Inhibition of human placental adenosine kinase |
CHEMBL1126884 |
| Adenosine kinase |
ED50 |
= |
0.008 |
uM |
Inhibition of adenosine kinase-induced MMPR (6-methylmercaptopurine riboside) toxicity in human CEM lymphoblasts |
CHEMBL1126884 |
| CCRF-CEM |
ID50 |
= |
0.9 |
uM |
Inhibition of human CEM lymphoblast proliferation |
CHEMBL1126884 |
| Rattus norvegicus |
Exudate |
= |
1.0 |
ml |
Antiinflammatory activity was measured 4 hr after administration of carrageenan at a oral dose of 2.5 mg / kg administered 1 hr before intrapleural injection of carrageenan in rat |
CHEMBL1126884 |
| Rattus norvegicus |
Change |
= |
40.0 |
% |
Percent change was reported in In vivo oral antiinflammatory activity in the rat carrageenan-induced pleurisy model (p<0.01) |
CHEMBL1126884 |
| Rattus norvegicus |
Activity |
= |
101000000.0 |
|
Total cells were calculated in the rat carrageenan-induced pleurisy model |
CHEMBL1126884 |
| Rattus norvegicus |
Change |
= |
43.0 |
% |
Percent change was reported in In vivo oral antiinflammatory activity in the rat carrageenan-induced pleurisy model |
CHEMBL1126884 |
| Adenosine kinase |
Ratio |
= |
115.0 |
|
Selectivity for adenosine kinase, Ratio of non-specific cellular (ID50) and specific MMPR-related (ED50) toxicity |
CHEMBL1126884 |
| HeLa |
MCC |
= |
1.0 |
ug.mL-1 |
Concentration required to cause a microscopically detectable alteration in cell morphology in HeLa cell cultures. |
CHEMBL1122581 |
| Vesicular stomatitis virus |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce vesicular stomatitis virus induced cytopathogenicity by 50% in HeLa cell cultures. |
CHEMBL1122581 |
| Human coxsackievirus B4 |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce coxsackie virus 4 induced cytopathogenicity by 50% in HeLa cell cultures. |
CHEMBL1122581 |
| Human poliovirus 1 |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce polio virus type 1 induced cytopathogenicity by 50% in HeLa cell cultures. |
CHEMBL1122581 |
| Vero |
MCC |
= |
1.0 |
ug.mL-1 |
Concentration required to cause a microscopically detectable alteration in cell morphology in vero cell cultures. |
CHEMBL1122581 |
| Mammalian orthoreovirus 1 |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce reovirus type 1 induced cytopathogenicity by 50% in vero cell cultures. |
CHEMBL1122581 |
| Human parainfluenza virus 3 |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce parainfluenza virus type 3 induced cytopathogenicity by 50% in vero cell cultures. |
CHEMBL1122581 |
| Sindbis virus |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce sindbis virus induced cytopathogenicity by 50% in vero cell cultures. |
CHEMBL1122581 |
| Human coxsackievirus B4 |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce coxsackie virus B4 induced cytopathogenicity by 50% in vero cell cultures. |
CHEMBL1122581 |
| Oryctolagus cuniculus |
MCC |
= |
1.0 |
ug.mL-1 |
Concentration required to cause a microscopically detectable alteration in cell morphology in primary rabbit kidney cell cultures. |
CHEMBL1122581 |
| Human herpesvirus 1 |
MIC |
= |
0.02 |
ug.mL-1 |
Concentration required to reduce HSV-1 (KOS) induced cytopathogenicity by 50% in primary rabbit kidney cell cultures. |
CHEMBL1122581 |
| Human herpesvirus 2 |
MIC |
> |
1.0 |
ug.mL-1 |
Concentration required to reduce HSV-2 (G) induced cytopathogenicity by 50% in primary rabbit kidney cell cultures. |
CHEMBL1122581 |
| Vaccinia virus |
MIC |
= |
0.07 |
ug.mL-1 |
Concentration required to reduce vaccinia virus induced cytopathogenicity by 50% in primary rabbit kidney cell cultures. |
CHEMBL1122581 |
| Vesicular stomatitis virus |
MIC |
> |
0.4 |
ug.mL-1 |
Concentration required to reduce vesicular stomatitis virus induced cytopathogenicity by 50% in primary rabbit kidney cell cultures. |
CHEMBL1122581 |
| L1210 |
ID50 |
= |
1.25 |
ug ml-1 |
Dose required to inhibit proliferation of L-1210 Cells by 50% |
CHEMBL1122581 |
| Adenosine kinase |
IC50 |
= |
26.0 |
nM |
Inhibition of human adenosine kinase activity |
CHEMBL1135244 |
| Adenosine kinase |
IC50 |
= |
38459178204.54 |
nM |
Inhibition concentration against human adenosine kinase |
CHEMBL1135244 |
| Adenosine kinase |
IC50 |
= |
26.0 |
nM |
Inhibitory activity against human recombinant adenosine kinase |
CHEMBL1136804 |
| Human herpesvirus 5 |
IC50 |
= |
400.0 |
nM |
Inhibitory concentration against human cytomegalovirus (HCMV) in plaque reduction assay |
CHEMBL1123999 |
| HFF |
IC50 |
= |
2000.0 |
nM |
Cytotoxicity against uninfected human foreskin fibroblast(HFF cells) |
CHEMBL1123999 |
| ADMET |
IC50 |
= |
2100.0 |
nM |
Cytotoxicity against human neoplastic cell line(KB cells) |
CHEMBL1123999 |
| Adenosine kinase |
IC50 |
= |
38904514499.43 |
nM |
Concentration required for 50% inhibition of the adenosine kinase (AK) activity. |
CHEMBL1137929 |
| Adenosine kinase |
IC50 |
= |
26.0 |
nM |
Inhibition of recombinant human adenosine kinase |
CHEMBL1133459 |
| Rattus norvegicus |
ED50 |
= |
6.0 |
mg.kg-1 |
Evaluated for antiseizure activity in rat maximal electric shock (MES) seizure model and represented as ED50. |
CHEMBL1133459 |
| Adenosine kinase |
IC50 |
= |
26.0 |
nM |
Inhibitory concentration against human recombinant adenosine kinase using [14C]AMP as radioligand |
CHEMBL1141114 |
| MAP kinase ERK2 |
Ki |
= |
530.0 |
nM |
Inhibition of ERK2 |
CHEMBL1145498 |
| Adenosine kinase |
Ki |
= |
30.0 |
nM |
Inhibition of adenosine kinase |
CHEMBL1145498 |
| Equilibrative nucleoside transporter 1 |
IC50 |
= |
229086.77 |
nM |
Binding affinity to ENT1 transporter |
CHEMBL1145549 |
| Adenosine kinase |
log(10'3/IC50) |
= |
4.59 |
|
Inhibition of adenosine kinase |
CHEMBL1157179 |
| Adenosine kinase |
logIC50 |
= |
-1.585 |
|
Inhibition of adenosine kinase (unknown origin) |
CHEMBL3046861 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Delta Tm |
= |
2.5 |
degrees C |
Binding affinity to human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) assessed as change in melting temperature at 50 uM by differential scanning fluorimetric analysis |
CHEMBL2346640 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
18200.0 |
nM |
Competitive inhibition of human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation counting analysis |
CHEMBL2346640 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
18000.0 |
nM |
Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor |
CHEMBL3085656 |
| AMP-activated protein kinase, alpha-2 subunit |
Thermal melting change |
= |
1.0 |
degrees C |
Delta TM value showing the stabilisation of AMPKA2 produced by compound binding |
CHEMBL1145498 |
| CaM kinase I delta |
Thermal melting change |
= |
0.2 |
degrees C |
Delta TM value showing the stabilisation of CAMK1D produced by compound binding |
CHEMBL1145498 |
| CaM kinase I gamma |
Thermal melting change |
= |
0.2 |
degrees C |
Delta TM value showing the stabilisation of CAMK1G produced by compound binding |
CHEMBL1145498 |
| CaM kinase II alpha |
Thermal melting change |
= |
0.7 |
degrees C |
Delta TM value showing the stabilisation of CAMK2A produced by compound binding |
CHEMBL1145498 |
| CaM kinase II beta |
Thermal melting change |
= |
0.4 |
degrees C |
Delta TM value showing the stabilisation of CAMK2B produced by compound binding |
CHEMBL1145498 |
| CaM kinase II delta |
Thermal melting change |
= |
-0.4 |
degrees C |
Delta TM value showing the stabilisation of CAMK2D produced by compound binding |
CHEMBL1145498 |
| CaM kinase II gamma |
Thermal melting change |
= |
0.6 |
degrees C |
Delta TM value showing the stabilisation of CAMK2G produced by compound binding |
CHEMBL1145498 |
| CaM kinase IV |
Thermal melting change |
= |
2.5 |
degrees C |
Delta TM value showing the stabilisation of CAMK4 produced by compound binding |
CHEMBL1145498 |
| CaM-kinase kinase beta |
Thermal melting change |
= |
2.0 |
degrees C |
Delta TM value showing the stabilisation of CAMKK2 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase 2 |
Thermal melting change |
= |
2.9 |
degrees C |
Delta TM value showing the stabilisation of CDK2 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase 6 |
Thermal melting change |
= |
-0.2 |
degrees C |
Delta TM value showing the stabilisation of CDK6 produced by compound binding |
CHEMBL1145498 |
| Cyclin-dependent kinase-like 1 |
Thermal melting change |
= |
0.2 |
degrees C |
Delta TM value showing the stabilisation of CDKL1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase Chk2 |
Thermal melting change |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of CHEK2 produced by compound binding |
CHEMBL1145498 |
| Dual specificty protein kinase CLK1 |
Thermal melting change |
= |
9.5 |
degrees C |
Delta TM value showing the stabilisation of CLK1 produced by compound binding |
CHEMBL1145498 |
| Dual specificity protein kinase CLK2 |
Thermal melting change |
= |
5.6 |
degrees C |
Delta TM value showing the stabilisation of CLK2 produced by compound binding |
CHEMBL1145498 |
| Dual specificity protein kinase CLK3 |
Thermal melting change |
= |
7.3 |
degrees C |
Delta TM value showing the stabilisation of CLK3 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I gamma 1 |
Thermal melting change |
= |
2.5 |
degrees C |
Delta TM value showing the stabilisation of CK1G1 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I gamma 2 |
Thermal melting change |
= |
3.7 |
degrees C |
Delta TM value showing the stabilisation of CK1G2 produced by compound binding |
CHEMBL1145498 |
| Casein kinase I isoform gamma-3 |
Thermal melting change |
= |
2.7 |
degrees C |
Delta TM value showing the stabilisation of CK1G3 produced by compound binding |
CHEMBL1145498 |
| Death-associated protein kinase 3 |
Thermal melting change |
= |
2.9 |
degrees C |
Delta TM value showing the stabilisation of DAPK3 produced by compound binding |
CHEMBL1145498 |
| Myotonin-protein kinase |
Thermal melting change |
= |
-0.3 |
degrees C |
Delta TM value showing the stabilisation of DMPK1 produced by compound binding |
CHEMBL1145498 |
| Glycogen synthase kinase-3 beta |
Thermal melting change |
= |
2.0 |
degrees C |
Delta TM value showing the stabilisation of GSK3B produced by compound binding |
CHEMBL1145498 |
| Tyrosine-protein kinase JAK1 |
Thermal melting change |
= |
0.2 |
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 |
= |
1.9 |
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 |
= |
2.7 |
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 |
= |
0.9 |
degrees C |
Delta TM value showing the stabilisation of ASK1 produced by compound binding |
CHEMBL1145498 |
| MAP kinase p38 beta |
Thermal melting change |
= |
-0.4 |
degrees C |
Delta TM value showing the stabilisation of p38beta produced by compound binding |
CHEMBL1145498 |
| MAP kinase ERK1 |
Thermal melting change |
= |
1.5 |
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 |
= |
1.4 |
degrees C |
Delta TM value showing the stabilisation of MST4(1) produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase NEK2 |
Thermal melting change |
= |
0.4 |
degrees C |
Delta TM value showing the stabilisation of NEK2 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase NEK6 |
Thermal melting change |
= |
-0.2 |
degrees C |
Delta TM value showing the stabilisation of NEK6 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase OSR1 |
Thermal melting change |
= |
2.4 |
degrees C |
Delta TM value showing the stabilisation of OSR1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK 4 |
Thermal melting change |
= |
1.1 |
degrees C |
Delta TM value showing the stabilisation of PAK4 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK7 |
Thermal melting change |
= |
0.7 |
degrees C |
Delta TM value showing the stabilisation of PAK5 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PAK6 |
Thermal melting change |
= |
1.1 |
degrees C |
Delta TM value showing the stabilisation of PAK6 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PCTAIRE-1 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of PCTK1 produced by compound binding |
CHEMBL1145498 |
| 3-phosphoinositide dependent protein kinase-1 |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of PDK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM1 |
Thermal melting change |
= |
1.1 |
degrees C |
Delta TM value showing the stabilisation of PIM1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM2 |
Thermal melting change |
= |
1.0 |
degrees C |
Delta TM value showing the stabilisation of PIM2 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PIM3 |
Thermal melting change |
= |
1.5 |
degrees C |
Delta TM value showing the stabilisation of PIM3 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PLK1 |
Thermal melting change |
= |
1.0 |
degrees C |
Delta TM value showing the stabilisation of PLK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase PLK4 |
Thermal melting change |
= |
2.9 |
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 |
= |
1.3 |
degrees C |
Delta TM value showing the stabilisation of PRKACA produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase RIO2 |
Thermal melting change |
= |
1.7 |
degrees C |
Delta TM value showing the stabilisation of RIOK2 produced by compound binding |
CHEMBL1145498 |
| Ribosomal protein S6 kinase alpha 3 |
Thermal melting change |
= |
1.7 |
degrees C |
Delta TM value showing the stabilisation of RSK2a produced by compound binding |
CHEMBL1145498 |
| Ribosomal protein S6 kinase alpha 3 |
Thermal melting change |
= |
1.4 |
degrees C |
Delta TM value showing the stabilisation of RSK2b produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 2 |
Thermal melting change |
= |
4.2 |
degrees C |
Delta TM value showing the stabilisation of SLK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 10 |
Thermal melting change |
= |
4.7 |
degrees C |
Delta TM value showing the stabilisation of LOK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 16 |
Thermal melting change |
= |
3.9 |
degrees C |
Delta TM value showing the stabilisation of MPSK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 17A |
Thermal melting change |
= |
2.8 |
degrees C |
Delta TM value showing the stabilisation of DRAK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 38 |
Thermal melting change |
= |
1.7 |
degrees C |
Delta TM value showing the stabilisation of NDR1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase MST4 |
Thermal melting change |
= |
2.1 |
degrees C |
Delta TM value showing the stabilisation of MST4 (2) produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase MST1 |
Thermal melting change |
= |
4.7 |
degrees C |
Delta TM value showing the stabilisation of MST1 produced by compound binding |
CHEMBL1145498 |
| TRAF2- and NCK-interacting kinase |
Thermal melting change |
= |
1.6 |
degrees C |
Delta TM value showing the stabilisation of TNIK produced by compound binding |
CHEMBL1145498 |
| PDZ-binding kinase |
Thermal melting change |
= |
0.0 |
degrees C |
Delta TM value showing the stabilisation of PBK produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase VRK1 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of VRK1 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase VRK2 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of VRK2 produced by compound binding |
CHEMBL1145498 |
| Inactive serine/threonine-protein kinase VRK3 |
Thermal melting change |
= |
0.1 |
degrees C |
Delta TM value showing the stabilisation of VRK3 produced by compound binding |
CHEMBL1145498 |
| Serine/threonine-protein kinase 25 |
Thermal melting change |
= |
4.2 |
degrees C |
Delta TM value showing the stabilisation of YSK1 produced by compound binding |
CHEMBL1145498 |
| MAP kinase ERK2 |
IC50 |
= |
1200.0 |
nM |
Inhibition of ERK2 (unknown origin) by ELISA |
CHEMBL3751810 |
| MAP kinase ERK2 |
Activity |
|
|
|
Displacement of p-nitroaniline labeled PEP from GST-fused ERK2 (unknown origin) |
CHEMBL3751810 |
| Adenosine kinase |
FC |
= |
200.0 |
|
Binding affinity to Toxoplasma gondii adenosine kinase assessed as formation of [14C]AMP from [14C]adenosine and ATP after 10 mins by liquid scintillation counting method relative to control |
CHEMBL3792305 |
| Plasmodium falciparum |
IC50 |
= |
2000.0 |
nM |
Antimalarial activity against synchronized Plasmodium falciparum ring stage form assessed as reduction in [2,8-3H]Hypoxanthine incorporation incubated for 48 hrs followed by addition of [2,8-3H]Hypoxanthine and measured after 24 hrs by liquid scintillation counting method |
CHEMBL4376805 |
| Adenosine kinase |
IC50 |
= |
1200.0 |
nM |
Inhibition of wild-type N-terminal TEV cleavage site-fused/His-tagged Mycobacterium tuberculosis H37Rv adenosine kinase expressed in Escherichia coli BL21 (DE3) using adenosine as substrate in presence of ATP and PEP by pyruvate kinase-lactate dehydrogenase coupled UV-vis spectrophotometric method |
CHEMBL4393679 |
| Adenosine kinase |
Ki |
= |
30.0 |
nM |
Inhibition of purified human adenosine kinase using varying levels of [3H]Ado as substrate in presence of adenosine deaminase inhibitor deoxycoformycin by Line-weaver burk plot analysis |
CHEMBL4393679 |
| Adenosine kinase |
Ki |
= |
210.0 |
nM |
Inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 adenosine kinase using varying levels of [3H]Ado as substrate in presence of adenosine deaminase inhibitor deoxycoformycin by Line-weaver burk plot analysis |
CHEMBL4393679 |
| Mycobacterium tuberculosis |
MIC |
= |
18000.0 |
nM |
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by micro plate alamar blue assay |
CHEMBL4393679 |
| Mycobacterium tuberculosis |
MIC |
> |
100000.0 |
nM |
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring D251N mutant by microplate alamar blue assay |
CHEMBL4393679 |
| Mycobacterium tuberculosis |
MIC |
> |
100000.0 |
nM |
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring Q172P mutant by microplate alamar blue assay |
CHEMBL4393679 |
| Mycobacterium tuberculosis |
MIC |
> |
100000.0 |
nM |
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring G262S mutant by microplate alamar blue assay |
CHEMBL4393679 |
| Trypanosoma cruzi |
EC50 |
= |
800.0 |
nM |
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells incubated for 7 days by chlorophenol red beta-D-galactopyranoside substrate based spectrophotometric assay |
CHEMBL4414577 |
| Unchecked |
EC50 |
= |
5350.0 |
nM |
Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based assay |
CHEMBL4414577 |
| Unchecked |
Ratio EC50 |
= |
6.7 |
|
Selectivity index, ratio for EC50 for human MRC5 SV2 cells to EC50 for Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells |
CHEMBL4414577 |
| Adenosine kinase |
IC50 |
= |
820.0 |
nM |
Inhibition of human adenosine kinase assessed as effect on reduced nicotinamide-adenine dinculeotide appearance using inosine as substrate in presence of NAD, ATP incubated for 4 hrs by IMPDH based coupled enzymatic assay based non-isotopic method |
CHEMBL4428046 |
| Adenosine kinase |
Inhibition |
= |
21.5 |
% |
Inhibition of human adenosine kinase assessed as effect on reduced nicotinamide-adenine dinculeotide appearance at 100 nM using inosine as substrate in presence of NAD, ATP incubated for 4 hrs by IMPDH based coupled enzymatic assay based non-isotopic method |
CHEMBL4428046 |
| Adenosine kinase |
Inhibition |
= |
44.4 |
% |
Inhibition of human adenosine kinase assessed as effect on reduced nicotinamide-adenine dinculeotide appearance at 500 nM using inosine as substrate in presence of NAD, ATP incubated for 4 hrs by IMPDH based coupled enzymatic assay based non-isotopic method |
CHEMBL4428046 |
| Adenosine kinase |
Inhibition |
= |
88.3 |
% |
Inhibition of human adenosine kinase assessed as effect on reduced nicotinamide-adenine dinculeotide appearance at 20 uM using inosine as substrate in presence of NAD, ATP incubated for 4 hrs by IMPDH based coupled enzymatic assay based non-isotopic method |
CHEMBL4428046 |
| Adenosine kinase |
Inhibition |
= |
88.3 |
% |
Inhibition of human adenosine kinase assessed as effect on reduced nicotinamide-adenine dinculeotide appearance at 50 uM using inosine as substrate in presence of NAD, ATP incubated for 4 hrs by IMPDH based coupled enzymatic assay based non-isotopic method |
CHEMBL4428046 |
| Adenosine kinase |
IC50 |
= |
26.0 |
nM |
Inhibition of human adenosine kinase assessed as reduction in conversion of adenosine to AMP |
CHEMBL4428046 |
| Adenosine kinase |
Inhibition |
|
|
% |
Inhibition of Adk in human 1321N cells assessed as [3H]AMP formation at 10 uM measured after 30 mins using [3H]adenosine by liquid scintillation counting method |
CHEMBL4428096 |
| Adenosine kinase |
Ki |
= |
9.3 |
nM |
Inhibition of Sprague-Dawley rat brain cytosolic Adk using [2-3H]adenosine incubated for 15 mins by scintillation spectrometry |
CHEMBL4428096 |
| Adenosine kinase |
Ki |
= |
26.0 |
nM |
Inhibition of recombinant human Adk using [U-14C]adenosine by liquid scintillation counting method |
CHEMBL4428096 |
| Adenosine kinase |
Ki |
= |
17.0 |
nM |
Inhibition of rat brain ADK expressed in Escherichia coli |
CHEMBL4428096 |
| Adenosine kinase |
Ki |
= |
16.3 |
nM |
Reversible inhibition of recombinant human Adk-short expressed in Escherichia coli BL21[DE3] assessed as [3H]AMP formation preincubated for 15 mins followed by [3H]adenosine addition measured after 30 mins by liquid scintillation counting method |
CHEMBL4428096 |
| Adenosine kinase |
Inhibition |
|
|
% |
Reversible inhibition of recombinant human Adk-short expressed in Escherichia coli BL21[DE3] assessed as [3H]AMP formation preincubated for 15 mins followed by [3H]adenosine addition measured after 30 mins by liquid scintillation counting method |
CHEMBL4428096 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
7000.0 |
nM |
Inhibition of DOT1L (unknown origin) using chicken nucleosome as substrate in presence of [3H]SAM incubated for 1 hr by TopCount method |
CHEMBL4477246 |
| Replicase polyprotein 1ab |
Inhibition |
= |
11.13 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
1.49 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| Glycogen synthase kinase-3 beta |
IC50 |
> |
50000.0 |
nM |
Inhibition of GSK3beta (unknown origin) |
CHEMBL4602691 |
| Pancreatic beta cells |
EC50 |
= |
460.0 |
nM |
Induction of cell proliferation in rat beta cells |
CHEMBL4602691 |
| Pancreatic beta cells |
Efficacy |
= |
11.0 |
% |
Induction of cell proliferation in rat beta cells relative to control |
CHEMBL4602691 |
| Dual-specificity tyrosine-phosphorylation regulated kinase 1A |
IC50 |
= |
71.0 |
nM |
Inhibition of DYRK1A (unknown origin) |
CHEMBL4602691 |
| Pancreatic beta cells |
EC50 |
= |
310.0 |
nM |
Induction of cell proliferation in human beta cells |
CHEMBL4602691 |
| Pancreatic beta cells |
Efficacy |
= |
56.0 |
% |
Induction of cell proliferation in human beta cells relative to control |
CHEMBL4602691 |
| SARS-CoV-2 |
Inhibition |
= |
1.49 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| Unchecked |
Delta Tm |
= |
4.0 |
degrees C |
Selective index, difference between deltaTm for recombinant wild type CLK1 (H148 to I484 residues) (unknown origin) expressed in Escherichia coli to deltaTm for recombinant CLK1 V324A mutant (unknown origin) expressed in Escherichia coli |
CHEMBL4725345 |
| Unchecked |
Delta Tm |
= |
4.0 |
degrees C |
Selective index, difference between deltaTm for CLK3 A319V mutant (unknown origin) expressed in Escherichia coli to deltaTm for recombinant wild type CLK3 (R134 to T484 residues) (unknown origin) expressed in Escherichia coli |
CHEMBL4725345 |
