Assay Detail
ADMET
CHEMBL4197033
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Inhibition of human CDK1/Cyclin-B using ULight-substrate after 1 hr by LANCE assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Cyclin-dependent kinase 1/cyclin B1 (CHEMBL1907602) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.18 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4213744 | — | — | 1 | 8.11 |
| CHEMBL4209352 | — | — | 1 | 7.91 |
| CHEMBL4216664 | — | — | 1 | 7.91 |
| CHEMBL4204483 | — | — | 1 | 7.40 |
| CHEMBL4206061 | — | — | 1 | 6.63 |
| CHEMBL4213219 | — | — | 1 | 6.50 |
| CHEMBL4204986 | — | — | 1 | 6.49 |
| CHEMBL4218588 | — | — | 1 | 6.45 |
| CHEMBL4212532 | — | — | 1 | 6.41 |
| CHEMBL4208813 | — | — | 1 | 6.33 |
| CHEMBL4212540 | — | — | 1 | 6.31 |
| CHEMBL4213756 | — | — | 1 | 6.29 |
| CHEMBL4210944 | — | — | 1 | 6.21 |
| CHEMBL4210422 | — | — | 1 | 6.18 |
| CHEMBL4207521 | — | — | 1 | 6.04 |
| CHEMBL4202644 | — | — | 1 | 6.01 |
| CHEMBL4214827 | — | — | 1 | 6.00 |
| CHEMBL4203179 | — | — | 1 | 5.93 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 5.83 |
| CHEMBL4210299 | — | — | 1 | 5.83 |
| CHEMBL4205132 | — | — | 1 | 5.74 |
| CHEMBL4202467 | — | — | 1 | 5.72 |
| CHEMBL4207796 | — | — | 1 | 5.63 |
| CHEMBL4210282 | — | — | 1 | 5.32 |
| CHEMBL4217628 | — | — | 1 | 5.29 |
| CHEMBL4214156 | — | — | 1 | 4.94 |
| CHEMBL4213778 | — | — | 1 | 4.87 |
| CHEMBL4205920 | — | — | 1 | 4.81 |
| CHEMBL4203758 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4213744 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4209352 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL4216664 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4204483 | — | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL4206061 | — | IC50 | = | 236.4 | nM | 6.63 |
| CHEMBL4213219 | — | IC50 | = | 319.8 | nM | 6.50 |
| CHEMBL4204986 | — | IC50 | = | 327.5 | nM | 6.49 |
| CHEMBL4218588 | — | IC50 | = | 355.2 | nM | 6.45 |
| CHEMBL4212532 | — | IC50 | = | 388.5 | nM | 6.41 |
| CHEMBL4208813 | — | IC50 | = | 466.6 | nM | 6.33 |
| CHEMBL4212540 | — | IC50 | = | 486.7 | nM | 6.31 |
| CHEMBL4213756 | — | IC50 | = | 507.1 | nM | 6.29 |
| CHEMBL4210944 | — | IC50 | = | 615.4 | nM | 6.21 |
| CHEMBL4210422 | — | IC50 | = | 666.7 | nM | 6.18 |
| CHEMBL4207521 | — | IC50 | = | 908.2 | nM | 6.04 |
| CHEMBL4202644 | — | IC50 | = | 976.0 | nM | 6.01 |
| CHEMBL4214827 | — | IC50 | = | 1003.0 | nM | 6.00 |
| CHEMBL4203179 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1487.0 | nM | 5.83 |
| CHEMBL4210299 | — | IC50 | = | 1464.0 | nM | 5.83 |
| CHEMBL4205132 | — | IC50 | = | 1828.0 | nM | 5.74 |
| CHEMBL4202467 | — | IC50 | = | 1921.0 | nM | 5.72 |
| CHEMBL4207796 | — | IC50 | = | 2353.0 | nM | 5.63 |
| CHEMBL4210282 | — | IC50 | = | 4828.0 | nM | 5.32 |
| CHEMBL4217628 | — | IC50 | = | 5082.0 | nM | 5.29 |
| CHEMBL4214156 | — | IC50 | = | 11495.0 | nM | 4.94 |
| CHEMBL4213778 | — | IC50 | = | 13510.0 | nM | 4.87 |
| CHEMBL4205920 | — | IC50 | = | 15565.0 | nM | 4.81 |
| CHEMBL4203758 | — | IC50 | > | 10000.0 | nM | - |