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Assay Detail

CHEMBL1815968

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of MIP-1alpha from human CCR5 expressed in CHO cells
1
Total Activities
1
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

Target

C-C chemokine receptor type 5 (CHEMBL274)
Type SINGLE PROTEIN
Organism Homo sapiens

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.
Nishizawa R, Nishiyama T, Hisaichi K, Minamoto C, Murota M, Takaoka Y, Nakai H, Tada H, Sagawa K, Shibayama S, Fukushima D, Maeda K, Mitsuya H.
Bioorg Med Chem (2011) 19 : 4028 -4042
PubMed 21658961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.24 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668019 APLAVIROC HYDROCHLORIDE 3.0 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668019 APLAVIROC HYDROCHLORIDE IC50 = 5.8 nM 8.24