Assay Detail
Binding
CHEMBL950060
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Inhibition of recombinant Chk1
23
Total Activities
23
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
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.31 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270181 | — | — | 1 | 9.24 |
| CHEMBL404189 | — | — | 1 | 9.22 |
| CHEMBL256193 | — | — | 1 | 9.15 |
| CHEMBL410195 | — | — | 1 | 9.05 |
| CHEMBL256192 | — | — | 1 | 9.01 |
| CHEMBL270417 | — | — | 1 | 8.72 |
| CHEMBL255183 | — | — | 1 | 8.59 |
| CHEMBL404152 | — | — | 1 | 8.51 |
| CHEMBL403192 | — | — | 1 | 8.47 |
| CHEMBL257067 | — | — | 1 | 8.46 |
| CHEMBL257703 | — | — | 1 | 8.40 |
| CHEMBL404479 | — | — | 1 | 8.40 |
| CHEMBL272347 | — | — | 1 | 8.32 |
| CHEMBL257512 | — | — | 1 | 8.17 |
| CHEMBL272711 | — | — | 1 | 8.10 |
| CHEMBL411098 | — | — | 1 | 8.09 |
| CHEMBL257317 | — | — | 1 | 8.05 |
| CHEMBL389816 | — | — | 1 | 8.00 |
| CHEMBL271727 | — | — | 1 | 7.95 |
| CHEMBL404498 | — | — | 1 | 7.81 |
| CHEMBL427720 | — | — | 1 | 7.79 |
| CHEMBL255816 | — | — | 1 | 7.66 |
| CHEMBL404021 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270181 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL404189 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL256193 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL410195 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL256192 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL270417 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL255183 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL404152 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL403192 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL257067 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL257703 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL404479 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL272347 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL257512 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL272711 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL411098 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL257317 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL389816 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL271727 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL404498 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL427720 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL255816 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL404021 | — | IC50 | = | 1050.0 | nM | 5.98 |