Assay Detail
Binding
CHEMBL4188522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate 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 |
| Cell Type | Sf9 |
| 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 | 7.45 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4208172 | — | — | 1 | 9.05 |
| CHEMBL4217694 | — | — | 1 | 8.62 |
| CHEMBL4209329 | — | — | 1 | 8.43 |
| CHEMBL4215702 | — | — | 1 | 8.40 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.11 |
| CHEMBL4210707 | — | — | 1 | 7.95 |
| CHEMBL4211828 | — | — | 1 | 7.90 |
| CHEMBL4210028 | — | — | 1 | 7.80 |
| CHEMBL4205645 | — | — | 1 | 7.76 |
| CHEMBL4207474 | — | — | 1 | 7.73 |
| CHEMBL4207451 | — | — | 1 | 7.72 |
| CHEMBL4213847 | — | — | 1 | 7.66 |
| CHEMBL4212542 | — | — | 1 | 7.55 |
| CHEMBL4207804 | — | — | 1 | 7.44 |
| CHEMBL4211479 | — | — | 1 | 7.34 |
| CHEMBL4208366 | — | — | 1 | 7.34 |
| CHEMBL4215126 | — | — | 1 | 6.75 |
| CHEMBL4204961 | — | — | 1 | 6.61 |
| CHEMBL4214566 | — | — | 1 | 6.61 |
| CHEMBL4216447 | — | — | 1 | 6.57 |
| CHEMBL4209318 | — | — | 1 | 6.56 |
| CHEMBL4213109 | — | — | 1 | 6.47 |
| CHEMBL4215568 | — | — | 1 | 6.41 |
| CHEMBL4207966 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4208172 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4217694 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4209329 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4215702 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4210707 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4211828 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4210028 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4205645 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4207474 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL4207451 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4213847 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4212542 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4207804 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4211479 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4208366 | — | IC50 | = | 45.6 | nM | 7.34 |
| CHEMBL4215126 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4204961 | — | IC50 | = | 247.8 | nM | 6.61 |
| CHEMBL4214566 | — | IC50 | = | 244.1 | nM | 6.61 |
| CHEMBL4216447 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL4209318 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4213109 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL4215568 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4207966 | — | IC50 | = | 752.0 | nM | 6.12 |