Assay Detail
Binding
CHEMBL959242
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Inhibition of AKT1
46
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.07 | 9.00 |
| Ki | 12 | 9.32 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523586 | — | — | 2 | 10.52 |
| CHEMBL469590 | — | — | 2 | 10.40 |
| CHEMBL520788 | — | — | 2 | 10.30 |
| CHEMBL470597 | — | — | 2 | 10.22 |
| CHEMBL496690 | — | — | 2 | 10.22 |
| CHEMBL482536 | — | — | 2 | 10.00 |
| CHEMBL470598 | — | — | 2 | 9.10 |
| CHEMBL498052 | — | — | 1 | 9.00 |
| CHEMBL469591 | — | — | 1 | 8.70 |
| CHEMBL498051 | — | — | 1 | 8.70 |
| CHEMBL482537 | — | — | 2 | 8.70 |
| CHEMBL524998 | — | — | 2 | 8.52 |
| CHEMBL512480 | — | — | 1 | 8.52 |
| CHEMBL470410 | — | — | 1 | 8.52 |
| CHEMBL471059 | — | — | 1 | 8.40 |
| CHEMBL512858 | — | — | 1 | 8.22 |
| CHEMBL471034 | — | — | 1 | 8.22 |
| CHEMBL469781 | — | — | 1 | 8.10 |
| CHEMBL512135 | — | — | 2 | 8.10 |
| CHEMBL469802 | — | — | 1 | 8.10 |
| CHEMBL470596 | — | — | 1 | 8.00 |
| CHEMBL470192 | — | — | 1 | 7.80 |
| CHEMBL513019 | — | — | 1 | 7.70 |
| CHEMBL470620 | — | — | 1 | 7.70 |
| CHEMBL513728 | — | — | 2 | 7.70 |
| CHEMBL472291 | — | — | 1 | 7.60 |
| CHEMBL512305 | — | — | 1 | 7.60 |
| CHEMBL512148 | — | — | 1 | 7.40 |
| CHEMBL512672 | — | — | 1 | 7.40 |
| CHEMBL470200 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523586 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL469590 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL520788 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL496690 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL470597 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL482536 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL470598 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL496690 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL523586 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL498052 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL470598 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL470597 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL469590 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL482536 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL498051 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL469591 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL482537 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL482537 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL512480 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL470410 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL520788 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL524998 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL471059 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL524998 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL512858 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL471034 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL469802 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL512135 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL469781 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL470596 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL470192 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL513728 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL470620 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL513019 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL512135 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL472291 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL512305 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL513728 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL512148 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL512672 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL470200 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL469357 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL470202 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL469560 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL470409 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL469561 | — | IC50 | = | 250.0 | nM | 6.60 |