Assay Detail
Binding
CHEMBL1028096
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Inhibition of AKT-mediated GSK3-beta phosphorylation in human BT474 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BT-474 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 20 | 6.07 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523859 | — | — | 1 | 7.00 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.85 |
| CHEMBL494060 | — | — | 1 | 6.85 |
| CHEMBL453510 | — | — | 1 | 6.64 |
| CHEMBL521642 | — | — | 1 | 6.40 |
| CHEMBL1794066 | GSK-619487A | — | 1 | 6.25 |
| CHEMBL494088 | — | — | 1 | 6.00 |
| CHEMBL493874 | — | — | 1 | 5.98 |
| CHEMBL523523 | — | — | 1 | 5.95 |
| CHEMBL493269 | — | — | 1 | 5.82 |
| CHEMBL1794065 | GSK-554170A | — | 1 | 5.68 |
| CHEMBL523057 | — | — | 1 | 5.56 |
| CHEMBL493251 | — | — | 1 | 5.47 |
| CHEMBL494882 | — | — | 1 | 5.41 |
| CHEMBL493875 | — | — | 1 | 5.21 |
| CHEMBL522351 | — | — | 1 | - |
| CHEMBL445180 | — | — | 1 | - |
| CHEMBL450487 | — | — | 1 | - |
| CHEMBL1794064 | GSK-561866B | — | 1 | - |
| CHEMBL493250 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523859 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL494089 | GSK-690693 | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL494060 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL453510 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL521642 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1794066 | GSK-619487A | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL494088 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL493874 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL523523 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL493269 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL1794065 | GSK-554170A | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL523057 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL493251 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL494882 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL493875 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL522351 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL445180 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL450487 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1794064 | GSK-561866B | IC50 | - | — | - | |
| CHEMBL493250 | — | IC50 | > | 30000.0 | nM | - |