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Assay Detail

CHEMBL4157396

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

Functional
Antiviral activity against HIV1 expressing gag T371A mutant infected in human MT2 cells after 4 to 5 days by dual luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176).
Regueiro-Ren A, Swidorski JJ, Liu Z, Chen Y, Sin N, Sit SY, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Easter J, Beno BR, Arora V, Huang XS, Rahematpura S, Parker DD, Haskell R, Santone KS, Cockett MI, Krystal M, Meanwell NA, Jenkins S, Hanumegowda U, Dicker IB.
J Med Chem (2018) 61 : 7289 -7313
PubMed 30067361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.05 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827379 BMS-955176 2.0 1 8.70
CHEMBL4163247 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827379 BMS-955176 EC50 = 2.0 nM 8.70
CHEMBL4163247 EC50 = 40.0 nM 7.40