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Assay Detail

CHEMBL3227489

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

Binding
Displacement of [125I]-MIP-1alpha from CCR5 in rhesus monkey Chem-1 cell membranes after 120 mins by liquid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Cell Type Chem-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL3217397)
Type SINGLE PROTEIN
Organism Macaca mulatta

Publication

A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Yuan Y, Arnatt CK, El-Hage N, Dever SM, Jacob JC, Selley DE, Hauser KF, Zhang Y.
Medchemcomm (2013) 4 : 847 -851
PubMed 23682308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.72 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256907 MARAVIROC 4.0 1 9.62
CHEMBL3219780 1 7.82
CHEMBL3219779 1 6.82
CHEMBL3219777 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256907 MARAVIROC Ki = 0.24 nM 9.62
CHEMBL3219780 Ki = 15.3 nM 7.82
CHEMBL3219779 Ki = 151.0 nM 6.82
CHEMBL3219777 Ki = 239.0 nM 6.62