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Assay Detail

CHEMBL1697615

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

Functional
Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.
Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.
ACS Med Chem Lett (2010) 1 : 483 -487
PubMed 24900235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.32 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688243 INCB-9471 2.0 1 9.80
CHEMBL82301 VICRIVIROC 3.0 1 9.64
CHEMBL1688242 1 7.96
CHEMBL1688240 1 7.72
CHEMBL1688239 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688243 INCB-9471 IC50 = 0.16 nM 9.80
CHEMBL82301 VICRIVIROC IC50 = 0.23 nM 9.64
CHEMBL1688242 IC50 = 11.0 nM 7.96
CHEMBL1688240 IC50 = 19.0 nM 7.72
CHEMBL1688239 IC50 = 334.0 nM 6.48