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Assay Detail

CHEMBL4713818

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

Functional
Antiviral activity against wild type HIV-1 NL4-3 infected in MT-2 cells assessed as inhibition of viral replication in presence of 40% human serum and 27 mg/ml human serum albumin by luciferase reporter gene based multicycle replication assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition.
Swidorski JJ,Jenkins S,Hanumegowda U,Parker DD,Beno BR,Protack T,Ng A,Gupta A,Shanmugam Y,Dicker IB,Krystal M,Meanwell NA,Regueiro-Ren A
Bioorg Med Chem Lett (2021) 36 : 127823 -127823
PubMed 33508465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.00 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741251 1 8.30
CHEMBL4789757 1 8.30
CHEMBL4792897 1 8.24
CHEMBL4171754 1 8.21
CHEMBL4793139 1 8.18
CHEMBL4756268 1 8.17
CHEMBL4758648 1 8.15
CHEMBL4788357 1 8.05
CHEMBL3827379 BMS-955176 2.0 1 7.94
CHEMBL3775172 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741251 EC50 = 5.0 nM 8.30
CHEMBL4789757 EC50 = 5.0 nM 8.30
CHEMBL4792897 EC50 = 5.7 nM 8.24
CHEMBL4171754 EC50 = 6.1 nM 8.21
CHEMBL4793139 EC50 = 6.6 nM 8.18
CHEMBL4756268 EC50 = 6.8 nM 8.17
CHEMBL4758648 EC50 = 7.0 nM 8.15
CHEMBL4788357 EC50 = 8.9 nM 8.05
CHEMBL3827379 BMS-955176 EC50 = 11.5 nM 7.94
CHEMBL3775172 EC50 = 316.0 nM 6.50