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Assay Detail

CHEMBL4719352

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

Binding
Displacement of [125I]MIP-1alpha from CCR5 receptor in rhesus monkey membrane incubated for 120 mins by liquid scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
Arnatt CK,Falls BA,Yuan Y,Raborg TJ,Masvekar RR,El-Hage N,Selley DE,Nicola AV,Knapp PE,Hauser KF,Zhang Y
Bioorg Med Chem (2016) 24 : 5969 -5987
PubMed 27720326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.69 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256907 MARAVIROC 4.0 1 9.62
CHEMBL4795179 1 6.82
CHEMBL4748891 1 6.62
CHEMBL4799343 1 -
CHEMBL4761614 1 -
CHEMBL4800480 1 -
CHEMBL4761273 1 -
CHEMBL4761986 1 -
CHEMBL4797451 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256907 MARAVIROC Ki = 0.24 nM 9.62
CHEMBL4795179 Ki = 151.0 nM 6.82
CHEMBL4748891 Ki = 239.0 nM 6.62
CHEMBL4799343 Ki - -
CHEMBL4761614 Ki - -
CHEMBL4800480 Ki - -
CHEMBL4761273 Ki - -
CHEMBL4761986 Ki - -
CHEMBL4797451 Ki - -