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Assay Detail

CHEMBL3828995

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Binding
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.
Regueiro-Ren A, Liu Z, Chen Y, Sin N, Sit SY, Swidorski JJ, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Beno BR, Huang XS, Rahematpura S, Parker DD, Haskell R, Jenkins S, Santone KS, Cockett MI, Krystal M, Meanwell NA, Hanumegowda U, Dicker IB.
ACS Med Chem Lett (2016) 7 : 568 -572
PubMed 27326328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.31 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827026 1 8.24
CHEMBL3827839 1 8.06
CHEMBL3787468 1 7.37
CHEMBL3775172 1 6.98
CHEMBL404519 BEVIRIMAT 2.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827026 EC50 = 5.7 nM 8.24
CHEMBL3827839 EC50 = 8.7 nM 8.06
CHEMBL3787468 EC50 = 43.0 nM 7.37
CHEMBL3775172 EC50 = 105.0 nM 6.98
CHEMBL404519 BEVIRIMAT EC50 = 1291.0 nM 5.89