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Assay Detail

CHEMBL859207

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

Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
Seto M, Aikawa K, Miyamoto N, Aramaki Y, Kanzaki N, Takashima K, Kuze Y, Iizawa Y, Baba M, Shiraishi M.
J Med Chem (2006) 49 : 2037 -2048
PubMed 16539392 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 9.40 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105686 CENICRIVIROC MESYLATE 1.0 1 10.00
CHEMBL3085308 1 9.72
CHEMBL3085309 1 9.68
CHEMBL3085307 1 9.62
CHEMBL3085311 1 9.32
CHEMBL3085310 1 9.02
CHEMBL204821 1 9.00
CHEMBL41275 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105686 CENICRIVIROC MESYLATE IC50 = 0.1 nM 10.00
CHEMBL3085308 IC50 = 0.19 nM 9.72
CHEMBL3085309 IC50 = 0.21 nM 9.68
CHEMBL3085307 IC50 = 0.24 nM 9.62
CHEMBL3085311 IC50 = 0.48 nM 9.32
CHEMBL3085310 IC50 = 0.95 nM 9.02
CHEMBL204821 IC50 = 1.0 nM 9.00
CHEMBL41275 IC50 = 1.4 nM 8.85