Assay Detail
Binding
CHEMBL1019461
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Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
23
Total Activities
23
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 | Autocuration |
Publication
1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.11 | 9.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473558 | — | — | 1 | 9.86 |
| CHEMBL256907 | MARAVIROC | 4.0 | 1 | 9.70 |
| CHEMBL489513 | — | — | 1 | 9.42 |
| CHEMBL491319 | — | — | 1 | 9.32 |
| CHEMBL473759 | — | — | 1 | 9.29 |
| CHEMBL522259 | — | — | 1 | 9.08 |
| CHEMBL491679 | — | — | 1 | 8.89 |
| CHEMBL3085107 | — | — | 1 | 8.85 |
| CHEMBL474154 | — | — | 1 | 8.51 |
| CHEMBL515261 | — | — | 1 | 8.50 |
| CHEMBL472953 | — | — | 1 | 8.41 |
| CHEMBL523267 | — | — | 1 | 8.31 |
| CHEMBL491153 | — | — | 1 | 8.21 |
| CHEMBL491154 | — | — | 1 | 7.54 |
| CHEMBL491320 | — | — | 1 | 7.30 |
| CHEMBL473353 | — | — | 1 | 7.28 |
| CHEMBL489324 | — | — | 1 | 7.21 |
| CHEMBL473352 | — | — | 1 | 7.07 |
| CHEMBL473348 | — | — | 1 | 7.05 |
| CHEMBL514000 | — | — | 1 | 6.79 |
| CHEMBL489323 | — | — | 1 | 6.75 |
| CHEMBL489512 | — | — | 1 | 6.73 |
| CHEMBL491328 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473558 | — | IC50 | = | 0.137 | nM | 9.86 |
| CHEMBL256907 | MARAVIROC | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL489513 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL491319 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL473759 | — | IC50 | = | 0.513 | nM | 9.29 |
| CHEMBL522259 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL491679 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3085107 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL474154 | — | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL515261 | — | IC50 | = | 3.16 | nM | 8.50 |
| CHEMBL472953 | — | IC50 | = | 3.93 | nM | 8.41 |
| CHEMBL523267 | — | IC50 | = | 4.87 | nM | 8.31 |
| CHEMBL491153 | — | IC50 | = | 6.12 | nM | 8.21 |
| CHEMBL491154 | — | IC50 | = | 28.7 | nM | 7.54 |
| CHEMBL491320 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL473353 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL489324 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL473352 | — | IC50 | = | 85.3 | nM | 7.07 |
| CHEMBL473348 | — | IC50 | = | 89.2 | nM | 7.05 |
| CHEMBL514000 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL489323 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL489512 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL491328 | — | IC50 | = | 315.0 | nM | 6.50 |