Assay Detail
Functional
CHEMBL747666
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against muscarinic M3 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.59 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311795 | — | — | 1 | 6.14 |
| CHEMBL263555 | — | — | 1 | 5.04 |
| CHEMBL79061 | — | — | 1 | - |
| CHEMBL432170 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311795 | — | Ki | = | 716.0 | nM | 6.14 |
| CHEMBL263555 | — | Ki | = | 9089.0 | nM | 5.04 |
| CHEMBL79061 | — | Ki | > | 5300.0 | nM | - |
| CHEMBL432170 | — | Ki | > | 5300.0 | nM | - |