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Assay Detail

CHEMBL859209

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Functional
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
11
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MOLT-4
Confidence 8 — Homologous 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 6 8.83 9.70
IC90 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105686 CENICRIVIROC MESYLATE 1.0 2 9.70
CHEMBL3085307 1 8.85
CHEMBL3085311 2 8.68
CHEMBL3085309 2 8.64
CHEMBL204821 2 8.28
CHEMBL3085308 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105686 CENICRIVIROC MESYLATE IC50 = 0.2 nM 9.70
CHEMBL3085307 IC50 = 1.4 nM 8.85
CHEMBL3085311 IC50 = 2.1 nM 8.68
CHEMBL3085309 IC50 = 2.3 nM 8.64
CHEMBL204821 IC50 = 5.3 nM 8.28
CHEMBL2105686 CENICRIVIROC MESYLATE IC90 = 0.81 nM -
CHEMBL204821 IC90 = 860.0 nM -
CHEMBL3085311 IC90 = 19.0 nM -
CHEMBL3085309 IC90 = 11.0 nM -
CHEMBL3085308 IC50 < 1.6 nM -
CHEMBL3085308 IC90 = 10.0 nM -