Assay Detail
Binding
CHEMBL922239
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Inhibition of human Chk1
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.70 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388648 | BIS-IMIDE A | — | 1 | 7.70 |
| CHEMBL265446 | — | — | 1 | 7.62 |
| CHEMBL406938 | — | — | 1 | 7.29 |
| CHEMBL240747 | GRANULATIMIDE | — | 1 | 7.09 |
| CHEMBL413188 | ISOGRANULATIMIDE | — | 1 | 7.00 |
| CHEMBL243930 | — | — | 1 | 6.57 |
| CHEMBL244140 | — | — | 1 | 6.51 |
| CHEMBL259432 | — | — | 1 | 5.72 |
| CHEMBL265691 | — | — | 1 | 4.84 |
| CHEMBL264661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388648 | BIS-IMIDE A | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL265446 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL406938 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL240747 | GRANULATIMIDE | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL413188 | ISOGRANULATIMIDE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL243930 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL244140 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL259432 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL265691 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL264661 | — | IC50 | - | — | - |