Assay Detail
Binding
CHEMBL1000364
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Inhibition of Cdc2/cyclin B assessed as inhibition of histone H1 phosphorylation in human HT29 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 1/cyclin B1 (CHEMBL1907602) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.00 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411662 | — | — | 1 | 6.19 |
| CHEMBL508541 | — | — | 1 | 6.15 |
| CHEMBL462011 | — | — | 1 | 5.89 |
| CHEMBL529669 | — | — | 1 | 5.77 |
| CHEMBL472542 | — | — | 1 | - |
| CHEMBL511280 | — | — | 1 | - |
| CHEMBL517744 | — | — | 1 | - |
| CHEMBL460940 | — | — | 1 | - |
| CHEMBL512342 | — | — | 1 | - |
| CHEMBL511992 | — | — | 1 | - |
| CHEMBL471329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411662 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL508541 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL462011 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL529669 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL472542 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL511280 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL517744 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL460940 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL512342 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL511992 | — | IC50 | > | 3400.0 | nM | - |
| CHEMBL471329 | — | IC50 | > | 3400.0 | nM | - |