Assay Detail
Functional
CHEMBL1815967
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Antiviral activity against R5 tropic multidrug-resistant HIV1 MM infected PBMC assessed as inhibition of viral p24 antigen expression
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.05 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | 3.0 | 1 | 9.22 |
| CHEMBL82301 | VICRIVIROC | 3.0 | 1 | 8.52 |
| CHEMBL41275 | — | — | 1 | 7.85 |
| CHEMBL129 | ZIDOVUDINE | 4.0 | 1 | 6.60 |
| CHEMBL1813459 | — | — | 1 | - |
| CHEMBL1170878 | — | — | 1 | - |
| CHEMBL1813436 | — | — | 1 | - |
| CHEMBL584 | NELFINAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL82301 | VICRIVIROC | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL41275 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL129 | ZIDOVUDINE | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1813459 | — | IC50 | - | — | - | |
| CHEMBL1170878 | — | IC50 | - | — | - | |
| CHEMBL1813436 | — | IC50 | - | — | - | |
| CHEMBL584 | NELFINAVIR | IC50 | > | 1000.0 | nM | - |