Assay Detail
Binding
CHEMBL889241
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Inhibition of human Akt1
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 7.97 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379300 | A-443654 | — | 1 | 9.80 |
| CHEMBL226898 | — | — | 1 | 9.22 |
| CHEMBL229320 | — | — | 1 | 9.05 |
| CHEMBL227322 | — | — | 1 | 8.92 |
| CHEMBL226625 | — | — | 1 | 8.92 |
| CHEMBL227367 | — | — | 1 | 8.89 |
| CHEMBL226849 | — | — | 1 | 8.85 |
| CHEMBL229968 | — | — | 1 | 8.74 |
| CHEMBL226627 | — | — | 1 | 8.74 |
| CHEMBL390372 | — | — | 1 | 8.68 |
| CHEMBL227050 | — | — | 1 | 8.62 |
| CHEMBL226996 | — | — | 1 | 8.60 |
| CHEMBL388312 | — | — | 1 | 8.54 |
| CHEMBL375919 | — | — | 1 | 8.51 |
| CHEMBL375717 | — | — | 1 | 8.51 |
| CHEMBL227271 | — | — | 1 | 8.48 |
| CHEMBL229917 | — | — | 1 | 8.44 |
| CHEMBL227368 | — | — | 1 | 8.41 |
| CHEMBL427422 | — | — | 1 | 8.30 |
| CHEMBL229855 | — | — | 1 | 8.30 |
| CHEMBL229918 | — | — | 1 | 8.25 |
| CHEMBL229799 | — | — | 1 | 8.23 |
| CHEMBL376394 | — | — | 1 | 8.22 |
| CHEMBL226745 | — | — | 1 | 8.17 |
| CHEMBL226850 | — | — | 1 | 8.14 |
| CHEMBL226577 | — | — | 1 | 8.11 |
| CHEMBL229314 | — | — | 1 | 8.08 |
| CHEMBL438483 | — | — | 1 | 8.07 |
| CHEMBL227366 | — | — | 1 | 8.00 |
| CHEMBL427426 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379300 | A-443654 | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL226898 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL229320 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL227322 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL226625 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL227367 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL226849 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL229968 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL226627 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL390372 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL227050 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL226996 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL388312 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL375717 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL375919 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL227271 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL229917 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL227368 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL427422 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL229855 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL229918 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL229799 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL376394 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL226745 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL226850 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL226577 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL229314 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL438483 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL227366 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL427426 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL229800 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL229798 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL227323 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL226744 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL375716 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL379218 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL227326 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL226529 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL388311 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL389438 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL227324 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL229315 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL376118 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL229854 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL390371 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL388809 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL227051 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL227325 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL226798 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL376792 | — | IC50 | = | 49.0 | nM | 7.31 |