Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL954254

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

Functional
Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in human CEM cells assessed as protection against virus-induced cytopathicity
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Piscitelli F, Coluccia A, Brancale A, La Regina G, Sansone A, Giordano C, Balzarini J, Maga G, Zanoli S, Samuele A, Cirilli R, La Torre F, Lavecchia A, Novellino E, Silvestri R.
J Med Chem (2009) 52 : 1922 -1934
PubMed 19281225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.15 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127012 1 6.18
CHEMBL126603 1 6.16
CHEMBL223228 EFAVIRENZ 4.0 1 6.12
CHEMBL469985 1 -
CHEMBL470007 1 -
CHEMBL502565 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127012 IC50 = 660.0 nM 6.18
CHEMBL126603 IC50 = 690.0 nM 6.16
CHEMBL223228 EFAVIRENZ IC50 = 760.0 nM 6.12
CHEMBL469985 IC50 >= 1000.0 nM -
CHEMBL470007 IC50 > 1000.0 nM -
CHEMBL502565 IC50 > 1000.0 nM -
CHEMBL57 NEVIRAPINE IC50 > 10000.0 nM -