Assay Detail
Functional
CHEMBL4188523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
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 | 8 | 5.88 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.72 |
| CHEMBL4208172 | — | — | 1 | 6.63 |
| CHEMBL4211828 | — | — | 1 | 5.94 |
| CHEMBL4212542 | — | — | 1 | 5.68 |
| CHEMBL4207474 | — | — | 1 | 5.67 |
| CHEMBL4213847 | — | — | 1 | 5.60 |
| CHEMBL4217694 | — | — | 1 | 5.58 |
| CHEMBL4207804 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4208172 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4211828 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL4212542 | — | IC50 | = | 2108.0 | nM | 5.68 |
| CHEMBL4207474 | — | IC50 | = | 2126.0 | nM | 5.67 |
| CHEMBL4213847 | — | IC50 | = | 2527.0 | nM | 5.60 |
| CHEMBL4217694 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL4207804 | — | IC50 | = | 5560.0 | nM | 5.25 |