Assay Detail
Binding
CHEMBL860618
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Displacement of [125I]RANTES from CCR5 expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.38 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41275 | — | — | 1 | 8.85 |
| CHEMBL3085307 | — | — | 1 | 8.77 |
| CHEMBL3085309 | — | — | 1 | 8.77 |
| CHEMBL204821 | — | — | 1 | 8.72 |
| CHEMBL3085310 | — | — | 1 | 8.66 |
| CHEMBL3085308 | — | — | 1 | 8.62 |
| CHEMBL2105686 | CENICRIVIROC MESYLATE | 1.0 | 1 | 8.51 |
| CHEMBL3085313 | — | — | 1 | 8.33 |
| CHEMBL3085311 | — | — | 1 | 8.17 |
| CHEMBL3085312 | — | — | 1 | 7.60 |
| CHEMBL3085305 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41275 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3085307 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3085309 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL204821 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3085310 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3085308 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2105686 | CENICRIVIROC MESYLATE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3085313 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3085311 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3085312 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3085305 | — | IC50 | = | 67.0 | nM | 7.17 |