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Assay Detail

CHEMBL3097946

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

Functional
Antiviral activity against enfuvirtide-resistant HIV-1 NL4-3 harboring gp41 (36G)V38E/N42S mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA
4
Total Activities
4
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

Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
He XY, Lu L, Qiu J, Zou P, Yu F, Jiang XK, Li L, Jiang S, Liu S, Xie L.
Bioorg Med Chem (2013) 21 : 7539 -7548
PubMed 23673219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.53 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092874 1 5.57
CHEMBL3092872 1 5.56
CHEMBL3092878 1 5.47
CHEMBL525076 ENFUVIRTIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092874 IC50 = 2670.0 nM 5.57
CHEMBL3092872 IC50 = 2746.0 nM 5.56
CHEMBL3092878 IC50 = 3367.0 nM 5.47
CHEMBL525076 ENFUVIRTIDE IC50 > 2000.0 nM -