Assay Detail
Binding
CHEMBL4188524
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
3
Total Activities
3
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 |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 3 | 5.21 | 5.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 5.48 |
| CHEMBL4208172 | — | — | 1 | 5.20 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4208172 | — | IC50 | = | 6380.0 | nM | 5.20 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 10900.0 | nM | 4.96 |