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Assay Detail

CHEMBL1664693

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

Functional
Antiviral activity against HIV1 isolate 92US657 infected in human MT2 cells assessed as inhibition viral p24 antigen production after 4 days by ELISA
18
Total Activities
18
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, synthesis, and biological activity of novel 5-((arylfuran/1H-pyrrol-2-yl)methylene)-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-4-ones as HIV-1 fusion inhibitors targeting gp41.
Jiang S, Tala SR, Lu H, Abo-Dya NE, Avan I, Gyanda K, Lu L, Katritzky AR, Debnath AK.
J Med Chem (2011) 54 : 572 -579
PubMed 21190369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.72 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650931 1 6.50
CHEMBL1650934 1 6.50
CHEMBL1650935 1 6.32
CHEMBL583135 1 6.28
CHEMBL1650933 1 6.06
CHEMBL1650932 1 6.00
CHEMBL575309 1 5.97
CHEMBL1650930 1 5.82
CHEMBL1650921 1 5.66
CHEMBL227675 1 5.62
CHEMBL1650927 1 5.56
CHEMBL1650929 1 5.53
CHEMBL1650928 1 5.46
CHEMBL1650924 1 5.38
CHEMBL1650926 1 5.33
CHEMBL1650923 1 5.23
CHEMBL1650922 1 5.09
CHEMBL1650925 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650931 EC50 = 320.0 nM 6.50
CHEMBL1650934 EC50 = 320.0 nM 6.50
CHEMBL1650935 EC50 = 477.0 nM 6.32
CHEMBL583135 EC50 = 521.0 nM 6.28
CHEMBL1650933 EC50 = 870.0 nM 6.06
CHEMBL1650932 EC50 = 990.0 nM 6.00
CHEMBL575309 EC50 = 1075.0 nM 5.97
CHEMBL1650930 EC50 = 1500.0 nM 5.82
CHEMBL1650921 EC50 = 2170.0 nM 5.66
CHEMBL227675 EC50 = 2380.0 nM 5.62
CHEMBL1650927 EC50 = 2780.0 nM 5.56
CHEMBL1650929 EC50 = 2940.0 nM 5.53
CHEMBL1650928 EC50 = 3430.0 nM 5.46
CHEMBL1650924 EC50 = 4160.0 nM 5.38
CHEMBL1650926 EC50 = 4710.0 nM 5.33
CHEMBL1650923 EC50 = 5890.0 nM 5.23
CHEMBL1650922 EC50 = 8060.0 nM 5.09
CHEMBL1650925 EC50 = 20830.0 nM 4.68