| Phosphatidylinositol 4-kinase, PI4K |
IC50 |
= |
84400.0 |
nM |
Inhibitory activity (IC50) against human phosphatidylinositol 4-kinase at the ATP binding site |
CHEMBL1124860 |
| Phosphatidylinositol 4-kinase, PI4K |
Ki |
= |
57900.0 |
nM |
Binding affinity (Ki) against human phosphatidylinositol 4-kinase |
CHEMBL1124860 |
| Rattus norvegicus |
Inhibition |
= |
33.0 |
% |
Ability to protect Sprague-Dawley male rats against maximal electroshock-induced seizures (MES) intraperitoneally. Inhibition at 25 mg/kg |
CHEMBL1124289 |
| GABA-A receptor; anion channel |
IC50 |
= |
37000.0 |
nM |
Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor |
CHEMBL1124455 |
| Phosphodiesterase 3 |
IC50 |
> |
200000.0 |
nM |
Inhibition of phosphodiesterase 3 at 1 uM cAMP |
CHEMBL1130051 |
| Phosphodiesterase 4 |
IC50 |
= |
160000.0 |
nM |
Inhibition of phosphodiesterase 4 at 1 uM cAMP |
CHEMBL1130051 |
| Mus musculus |
MEC |
> |
10.0 |
uM |
Minimum effective concentration required for more than 1 IU/mL induction of IFN using mice spleen cells |
CHEMBL1135670 |
| Serine/threonine-protein kinase RAF |
Inhibition |
= |
25.0 |
% |
Inhibition of human RAF proto-oncogene serine/threonine-protein kinase at 30 uM |
CHEMBL1141882 |
| Dual specificity mitogen-activated protein kinase kinase 1 |
Inhibition |
= |
7.0 |
% |
Inhibition of human Mitogen activated protein kinase kinase 1 (MEK1) at 30 uM |
CHEMBL1141882 |
| cAMP-dependent protein kinase (PKA) |
Inhibition |
= |
1.0 |
% |
Inhibition of human cAMP-dependent protein kinase (PKA) |
CHEMBL1141882 |
| Serine/threonine-protein kinase AKT |
Inhibition |
= |
0.0 |
% |
Inhibition of human Protein kinase B alpha at 30 uM |
CHEMBL1141882 |
| Protein kinase C alpha |
Inhibition |
= |
2.0 |
% |
Inhibition of human Protein kinase C alpha |
CHEMBL1141882 |
| Rho-associated protein kinase 1 |
Inhibition |
= |
5.0 |
% |
Inhibition of human Rho-dependent protein kinase-II at 30 uM |
CHEMBL1141882 |
| MAP kinase p38 alpha |
Inhibition |
= |
7.0 |
% |
Inhibition of human stress-activated protein kinase-2 alpha (p38 MAP-kinase) at 30 uM |
CHEMBL1141882 |
| Ca2+/calmodulin-dependent protein kinase II (CaM kinase II) |
Inhibition |
= |
0.0 |
% |
Inhibition of rat Calcium/calmodulin-dependent protein kinase type II at 30 uM |
CHEMBL1141882 |
| Glycogen synthase kinase-3 beta |
Inhibition |
= |
7.0 |
% |
Inhibition of human Glycogen synthase kinase-3 beta at 30 uM |
CHEMBL1141882 |
| c-Jun N-terminal kinase 1 |
Inhibition |
= |
1.0 |
% |
Inhibition of human c-Jun N-terminal kinase-1 alpha-1 at 30 uM |
CHEMBL1141882 |
| c-Jun N-terminal kinase 2 |
Inhibition |
= |
0.0 |
% |
Inhibition of human c-Jun N-terminal kinase-2 alpha-2 at 30 uM |
CHEMBL1141882 |
| c-Jun N-terminal kinase 3 |
Inhibition |
= |
17.0 |
% |
Inhibition of rat c-Jun N-terminal kinase-3 at 30 uM |
CHEMBL1141882 |
| Tyrosine-protein kinase LCK |
Inhibition |
= |
19.0 |
% |
Inhibition of human lymphocyte protein tyrosine kinase Lck at 30 uM |
CHEMBL1141882 |
| MAP kinase ERK1 |
Inhibition |
= |
17.0 |
% |
Inhibition of human Mitogen-activated protein kinase 1 at 30 uM |
CHEMBL1141882 |
| MAP kinase ERK2 |
Inhibition |
= |
11.0 |
% |
Inhibition of human Mitogen-activated protein kinase 2 at 30 uM |
CHEMBL1141882 |
| Adenosine A1 receptor |
Ki |
> |
100000.0 |
nM |
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1153377 |
| Adenosine A2a receptor |
Ki |
= |
8500.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1153377 |
| Adenosine A2b receptor |
Ki |
> |
30000.0 |
nM |
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity |
CHEMBL1153377 |
| Adenosine A3 receptor |
Ki |
> |
100000.0 |
nM |
Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1153377 |
| Unchecked |
Ki |
> |
100000.0 |
nM |
Displacement of [3H]adenine from adenine 1 receptor in rat brain cortical membrane by liquid scintillation counting |
CHEMBL1156038 |
| Unchecked |
Inhibition |
= |
15.0 |
% |
Inhibition of [3H]adenine binding to adenine 1 receptor in rat brain cortical membrane at 100 uM by liquid scintillation counting |
CHEMBL1156038 |
| Plasmodium falciparum |
Potency |
|
18526.0 |
nM |
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488745, AID488752, AID488774, AID504848, AID504850] |
CHEMBL1201862 |
| DNA polymerase iota |
Potency |
|
28183.8 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of Polymerase Iota. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588623] |
CHEMBL1201862 |
| No relevant target |
Solubility |
|
245500.0 |
nM |
ASTRAZENECA: Solubility in pH7.4 buffer using solid starting material using the method described in J. Assoc. Lab. Autom. 2011, 16, 276-284. Experimental range 0.10 to 1500 uM |
CHEMBL3301361 |
| No relevant target |
LogD7.4 |
|
1.53 |
|
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 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of ATPgammaS-BODIPY binding to Thermotoga maritima His-tagged HK853 expressed in Escherichia coli BL21(DE3)pLysS Rosetta preincubated for 30 mins prior to ATPgammaS-BODIPY addition measured after 1 hr by coomassie staining-based SDS-PAGE analysis |
CHEMBL4017529 |
| 5'-nucleotidase |
Inhibition |
= |
23.0 |
% |
Inhibition of recombinant cN-II (unknown origin) assessed as reduction in inorganic phosphate production at 1 mM pre-incubated for 10 mins followed by addition of IMP as substrate and measured after 5 mins by malachite green based assay relative to control |
CHEMBL4387703 |
| RL |
IC50 |
> |
200000.0 |
nM |
Antiproliferative activity against human RL cells assessed as reduction in cell survival incubated for 72 hrs by MTT assay |
CHEMBL4387703 |
| Protein arginine N-methyltransferase 5 |
Inhibition |
= |
15.6 |
% |
Displacement of [3H]-SAM from PRMT5 (unknown origin) at 10 uM using peptide substrate preincubated for 15 mins followed by substrate addition for 60 mins by radioactive biochemical assay relative to control |
CHEMBL5154928 |
