Assay Detail
Binding
CHEMBL4188521
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Inhibition of CDK4 (unknown origin) after 90 mins by ADP-Glo assay
24
Total Activities
24
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 |
Publication
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.08 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211828 | — | — | 1 | 9.22 |
| CHEMBL4209329 | — | — | 1 | 9.22 |
| CHEMBL4215702 | — | — | 1 | 9.10 |
| CHEMBL4205645 | — | — | 1 | 9.00 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.77 |
| CHEMBL4210028 | — | — | 1 | 8.76 |
| CHEMBL4210707 | — | — | 1 | 8.24 |
| CHEMBL4209318 | — | — | 1 | 8.24 |
| CHEMBL4208366 | — | — | 1 | 8.17 |
| CHEMBL4208172 | — | — | 1 | 8.13 |
| CHEMBL4207451 | — | — | 1 | 8.01 |
| CHEMBL4217694 | — | — | 1 | 8.00 |
| CHEMBL4213847 | — | — | 1 | 7.85 |
| CHEMBL4215568 | — | — | 1 | 7.80 |
| CHEMBL4211479 | — | — | 1 | 7.80 |
| CHEMBL4207966 | — | — | 1 | 7.75 |
| CHEMBL4214566 | — | — | 1 | 7.75 |
| CHEMBL4207474 | — | — | 1 | 7.72 |
| CHEMBL4207804 | — | — | 1 | 7.70 |
| CHEMBL4216447 | — | — | 1 | 7.60 |
| CHEMBL4212542 | — | — | 1 | 7.57 |
| CHEMBL4215126 | — | — | 1 | 7.41 |
| CHEMBL4213109 | — | — | 1 | 7.30 |
| CHEMBL4204961 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211828 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4209329 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4215702 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4205645 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4210028 | — | IC50 | = | 1.72 | nM | 8.76 |
| CHEMBL4210707 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4209318 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4208366 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4208172 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4207451 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4217694 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4213847 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4215568 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4211479 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4207966 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL4214566 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4207474 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4207804 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4216447 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4212542 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4215126 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4213109 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL4204961 | — | IC50 | = | 147.3 | nM | 6.83 |