Assay Detail
Binding
CHEMBL949043
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Inhibition of Chk1
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.36 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272479 | — | — | 1 | 8.52 |
| CHEMBL271084 | — | — | 1 | 8.40 |
| CHEMBL270866 | — | — | 1 | 8.15 |
| CHEMBL271071 | — | — | 1 | 8.00 |
| CHEMBL255565 | — | — | 1 | 7.85 |
| CHEMBL255427 | — | — | 1 | 7.85 |
| CHEMBL258067 | — | — | 1 | 7.66 |
| CHEMBL272946 | — | — | 1 | 7.66 |
| CHEMBL410261 | — | — | 1 | 7.62 |
| CHEMBL256480 | — | — | 1 | 7.39 |
| CHEMBL404335 | — | — | 1 | 7.36 |
| CHEMBL214253 | — | — | 1 | 7.33 |
| CHEMBL401746 | — | — | 1 | 7.26 |
| CHEMBL402093 | — | — | 1 | 7.24 |
| CHEMBL270021 | — | — | 1 | 7.20 |
| CHEMBL403679 | — | — | 1 | 7.15 |
| CHEMBL438566 | — | — | 1 | 7.13 |
| CHEMBL255416 | — | — | 1 | 6.99 |
| CHEMBL401776 | — | — | 1 | 6.87 |
| CHEMBL411662 | — | — | 1 | 6.77 |
| CHEMBL257857 | — | — | 1 | 6.62 |
| CHEMBL272267 | — | — | 1 | 6.62 |
| CHEMBL271715 | — | — | 1 | 6.54 |
| CHEMBL272351 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272479 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL271084 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL270866 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL271071 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL255565 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL255427 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL258067 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL272946 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL410261 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL256480 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL404335 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL214253 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL401746 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL402093 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL270021 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL403679 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL438566 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL255416 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL401776 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL411662 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL257857 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL272267 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL271715 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL272351 | — | IC50 | = | 374.0 | nM | 6.43 |