Assay Detail
Binding
CHEMBL1697612
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]MIP-1beta from CCR5 in IL-10-stimulated human monocytes
10
Total Activities
9
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 |
Publication
Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.88 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL82301 | VICRIVIROC | 3.0 | 1 | 8.52 |
| CHEMBL1688239 | — | — | 2 | 8.41 |
| CHEMBL1688242 | — | — | 1 | 8.34 |
| CHEMBL1688240 | — | — | 1 | 8.30 |
| CHEMBL1688243 | INCB-9471 | 2.0 | 1 | 8.19 |
| CHEMBL1688241 | — | — | 1 | 6.68 |
| CHEMBL1688244 | — | — | 1 | - |
| CHEMBL1687948 | — | — | 1 | - |
| CHEMBL1688245 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL82301 | VICRIVIROC | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1688239 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1688242 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1688240 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1688243 | INCB-9471 | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1688239 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1688241 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL1688244 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1687948 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1688245 | — | IC50 | > | 1000.0 | nM | - |