Assay Detail
Binding
CHEMBL1016198
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Inhibition of CDK1/Cyclin B1 assessed as inhibition of retinoblastoma susceptibility gene product phosphorylation
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 1/cyclin B1 (CHEMBL1907602) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 4.83 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489853 | — | — | 1 | 5.60 |
| CHEMBL490240 | — | — | 1 | 5.51 |
| CHEMBL477259 | — | — | 1 | 5.51 |
| CHEMBL489245 | — | — | 1 | 5.22 |
| CHEMBL515631 | — | — | 1 | 5.21 |
| CHEMBL489039 | — | — | 1 | 5.09 |
| CHEMBL489629 | — | — | 1 | 5.02 |
| CHEMBL489445 | — | — | 1 | 5.01 |
| CHEMBL477863 | — | — | 1 | 5.00 |
| CHEMBL490451 | — | — | 1 | 4.94 |
| CHEMBL521922 | — | — | 1 | 4.87 |
| CHEMBL477063 | — | — | 1 | 4.83 |
| CHEMBL514678 | — | — | 1 | 4.79 |
| CHEMBL489246 | — | — | 1 | 4.65 |
| CHEMBL489646 | — | — | 1 | 4.63 |
| CHEMBL504547 | — | — | 1 | 4.61 |
| CHEMBL477064 | — | — | 1 | 4.60 |
| CHEMBL490251 | — | — | 1 | 4.53 |
| CHEMBL523780 | — | — | 1 | 4.46 |
| CHEMBL450383 | — | — | 1 | 4.44 |
| CHEMBL489627 | — | — | 1 | 4.43 |
| CHEMBL485502 | — | — | 1 | 4.37 |
| CHEMBL478488 | — | — | 1 | 4.32 |
| CHEMBL489430 | — | — | 1 | 4.31 |
| CHEMBL449818 | — | — | 1 | - |
| CHEMBL477877 | — | — | 1 | - |
| CHEMBL447758 | — | — | 1 | - |
| CHEMBL489432 | — | — | 1 | - |
| CHEMBL489631 | — | — | 1 | - |
| CHEMBL489030 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489853 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL490240 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL477259 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL489245 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL515631 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL489039 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL489629 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL489445 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL477863 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL490451 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL521922 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL477063 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL514678 | — | IC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL489246 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL489646 | — | IC50 | = | 23300.0 | nM | 4.63 |
| CHEMBL504547 | — | IC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL477064 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL490251 | — | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL523780 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL450383 | — | IC50 | = | 36600.0 | nM | 4.44 |
| CHEMBL489627 | — | IC50 | = | 37200.0 | nM | 4.43 |
| CHEMBL485502 | — | IC50 | = | 42500.0 | nM | 4.37 |
| CHEMBL478488 | — | IC50 | = | 47800.0 | nM | 4.32 |
| CHEMBL489430 | — | IC50 | = | 48700.0 | nM | 4.31 |
| CHEMBL477860 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL478487 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL502651 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL484477 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL484274 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL485503 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL520020 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL490053 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL489854 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL451298 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL452447 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL477861 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL477862 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL490241 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL489244 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL489030 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL489631 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL489432 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL447758 | — | IC50 | < | 50000.0 | nM | - |
| CHEMBL477877 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL449818 | — | IC50 | > | 5050000.0 | nM | - |