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Assay Detail

CHEMBL4148442

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

Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL3676)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Recent updates for designing CCR5 antagonists as anti-retroviral agents.
Shah HR, Savjani JK.
Eur J Med Chem (2018) 147 : 115 -129
PubMed 29425816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.97 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110727 CENICRIVIROC 3.0 1 9.60
CHEMBL1255794 APLAVIROC 3.0 1 9.40
CHEMBL82301 VICRIVIROC 3.0 1 9.04
CHEMBL1172035 NIFEVIROC 1 8.54
CHEMBL256907 MARAVIROC 4.0 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110727 CENICRIVIROC IC50 = 0.25 nM 9.60
CHEMBL1255794 APLAVIROC IC50 = 0.4 nM 9.40
CHEMBL82301 VICRIVIROC IC50 = 0.91 nM 9.04
CHEMBL1172035 NIFEVIROC IC50 = 2.9 nM 8.54
CHEMBL256907 MARAVIROC IC50 = 5.2 nM 8.28