Assay Detail
Binding
CHEMBL959243
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Inhibition of AKT-mediated GSK3-beta phosphorylation in human BT474 cells by mechanistic assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BT-474 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.15 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL520788 | — | — | 1 | 7.30 |
| CHEMBL469590 | — | — | 1 | 7.10 |
| CHEMBL523586 | — | — | 1 | 7.05 |
| CHEMBL470597 | — | — | 1 | 7.00 |
| CHEMBL469781 | — | — | 1 | 6.92 |
| CHEMBL482536 | — | — | 1 | 6.77 |
| CHEMBL496690 | — | — | 1 | 6.75 |
| CHEMBL471034 | — | — | 1 | 6.72 |
| CHEMBL498052 | — | — | 1 | 6.66 |
| CHEMBL470192 | — | — | 1 | 6.62 |
| CHEMBL469591 | — | — | 1 | 6.58 |
| CHEMBL512135 | — | — | 1 | 6.30 |
| CHEMBL512480 | — | — | 1 | 6.25 |
| CHEMBL470410 | — | — | 1 | 6.11 |
| CHEMBL512858 | — | — | 1 | 6.10 |
| CHEMBL524998 | — | — | 1 | 6.00 |
| CHEMBL512672 | — | — | 1 | 6.00 |
| CHEMBL512305 | — | — | 1 | 5.96 |
| CHEMBL471059 | — | — | 1 | 5.96 |
| CHEMBL469802 | — | — | 1 | 5.82 |
| CHEMBL498051 | — | — | 1 | 5.72 |
| CHEMBL470598 | — | — | 1 | 5.72 |
| CHEMBL482537 | — | — | 1 | 5.70 |
| CHEMBL470596 | — | — | 1 | 5.68 |
| CHEMBL470202 | — | — | 1 | 5.60 |
| CHEMBL472291 | — | — | 1 | 5.33 |
| CHEMBL513019 | — | — | 1 | 5.32 |
| CHEMBL513728 | — | — | 1 | 5.22 |
| CHEMBL469357 | — | — | 1 | 5.22 |
| CHEMBL470200 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL520788 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL469590 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL523586 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL470597 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL469781 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL482536 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL496690 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL471034 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL498052 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL470192 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL469591 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL512135 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL512480 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL470410 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL512858 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL524998 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL512672 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL512305 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL471059 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL469802 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL498051 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL470598 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL482537 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL470596 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL470202 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL472291 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL513019 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL513728 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL469357 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL470200 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL470620 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL512148 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL470409 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL469561 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL469560 | — | IC50 | > | 10000.0 | nM | - |