Assay Detail
Functional
CHEMBL745192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against Muscarinic acetylcholine receptor M2
7
Total Activities
7
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 | 7 | 5.61 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311795 | — | — | 1 | 6.34 |
| CHEMBL312344 | — | — | 1 | 5.45 |
| CHEMBL263555 | — | — | 1 | 5.32 |
| CHEMBL432170 | — | — | 1 | 5.32 |
| CHEMBL79061 | — | — | 1 | - |
| CHEMBL82301 | VICRIVIROC | 3.0 | 1 | - |
| CHEMBL80251 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311795 | — | Ki | = | 456.0 | nM | 6.34 |
| CHEMBL312344 | — | Ki | = | 3512.0 | nM | 5.45 |
| CHEMBL263555 | — | Ki | = | 4750.0 | nM | 5.32 |
| CHEMBL432170 | — | Ki | = | 4760.0 | nM | 5.32 |
| CHEMBL79061 | — | Ki | > | 5700.0 | nM | - |
| CHEMBL82301 | VICRIVIROC | Ki | > | 10000.0 | nM | - |
| CHEMBL80251 | — | Ki | > | 6700.0 | nM | - |