Assay Detail
Functional
CHEMBL1816014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat CCR5 assessed as inhibition of RANTES-induced calcium mobilization
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
C-C chemokine receptor type 5 (CHEMBL1795146) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 1 | 4.52 | 4.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | 3.0 | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | IC50 | = | 30000.0 | nM | 4.52 |