Assay Detail
Functional
CHEMBL815092
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Inhibition of the entry of HIV-1 reporter virus (ADA) into U-87 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.93 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113436 | — | — | 1 | 9.30 |
| CHEMBL113072 | — | — | 1 | 9.30 |
| CHEMBL113042 | — | — | 1 | 9.10 |
| CHEMBL115487 | — | — | 1 | 9.00 |
| CHEMBL322251 | — | — | 1 | 9.00 |
| CHEMBL115716 | — | — | 1 | 9.00 |
| CHEMBL113154 | — | — | 1 | 9.00 |
| CHEMBL325276 | — | — | 1 | 8.92 |
| CHEMBL326020 | — | — | 1 | 8.70 |
| CHEMBL111998 | — | — | 1 | 8.49 |
| CHEMBL112299 | — | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113436 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL113072 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL113042 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL115487 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL322251 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL115716 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL113154 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL325276 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL326020 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL111998 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL112299 | — | IC50 | = | 4.0 | nM | 8.40 |