Assay Detail
Binding
CHEMBL1028092
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Inhibition of human recombinant ROCK1 expressed in Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.73 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521823 | — | — | 1 | 8.52 |
| CHEMBL523695 | — | — | 1 | 8.30 |
| CHEMBL506153 | GW876790X | — | 1 | 8.30 |
| CHEMBL493911 | — | — | 1 | 8.10 |
| CHEMBL493066 | — | — | 1 | 7.70 |
| CHEMBL523523 | — | — | 1 | 7.70 |
| CHEMBL493067 | — | — | 1 | 7.40 |
| CHEMBL523057 | — | — | 1 | 6.90 |
| CHEMBL493875 | — | — | 1 | 6.90 |
| CHEMBL493251 | — | — | 1 | 6.80 |
| CHEMBL1794064 | GSK-561866B | — | 1 | 6.70 |
| CHEMBL450487 | — | — | 1 | 6.65 |
| CHEMBL522351 | — | — | 1 | 6.60 |
| CHEMBL493874 | — | — | 1 | 6.30 |
| CHEMBL493269 | — | — | 1 | 6.30 |
| CHEMBL453510 | — | — | 1 | 6.30 |
| CHEMBL445180 | — | — | 1 | 6.25 |
| CHEMBL494088 | — | — | 1 | 6.10 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.05 |
| CHEMBL1794066 | GSK-619487A | — | 1 | 6.00 |
| CHEMBL523859 | — | — | 1 | 5.90 |
| CHEMBL521642 | — | — | 1 | 5.80 |
| CHEMBL494882 | — | — | 1 | 5.70 |
| CHEMBL1794065 | GSK-554170A | — | 1 | 5.60 |
| CHEMBL494060 | — | — | 1 | 5.40 |
| CHEMBL493250 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521823 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL523695 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL506153 | GW876790X | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL493911 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL493066 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL523523 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL493067 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL523057 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL493875 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL493251 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL1794064 | GSK-561866B | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL450487 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL522351 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL493874 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL493269 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL453510 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL445180 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL494088 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL494089 | GSK-690693 | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1794066 | GSK-619487A | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL523859 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL521642 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL494882 | — | IC50 | = | 1995.0 | nM | 5.70 |
| CHEMBL1794065 | GSK-554170A | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL494060 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL493250 | — | IC50 | - | — | - |