Assay Detail
Functional
CHEMBL815078
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Compound was tested for inhibiting the entry of replication deffective HIV-1 (YU-2) in to U-80 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-80 |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| IC50 | 6 | 9.39 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79061 | — | — | 1 | 9.89 |
| CHEMBL263555 | — | — | 1 | 9.74 |
| CHEMBL311795 | — | — | 1 | 9.41 |
| CHEMBL82301 | VICRIVIROC | 3.0 | 1 | 9.34 |
| CHEMBL312344 | — | — | 1 | 9.10 |
| CHEMBL80251 | — | — | 1 | 8.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79061 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL263555 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL311795 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL82301 | VICRIVIROC | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL312344 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL80251 | — | IC50 | = | 1.44 | nM | 8.84 |