Assay Detail
Functional
CHEMBL649943
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Antagonistic activity against C-C chemokine receptor type 5
6
Total Activities
6
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 | 6 | 8.67 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432170 | — | — | 1 | 8.96 |
| CHEMBL79061 | — | — | 1 | 8.85 |
| CHEMBL312344 | — | — | 1 | 8.80 |
| CHEMBL82301 | VICRIVIROC | 3.0 | 1 | 8.60 |
| CHEMBL311795 | — | — | 1 | 8.55 |
| CHEMBL263555 | — | — | 1 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432170 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL79061 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL312344 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL82301 | VICRIVIROC | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL311795 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL263555 | — | Ki | = | 5.2 | nM | 8.28 |