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Assay Detail

CHEMBL2169129

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

Functional
Antiviral activity against HIV-1 harboring reverse transcriptase K101E mutant infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type TZM-bl
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
Sun LQ, Zhu L, Qian K, Qin B, Huang L, Chen CH, Lee KH, Xie L.
J Med Chem (2012) 55 : 7219 -7229
PubMed 22856541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.13 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165299 1 8.47
CHEMBL2012795 1 8.47
CHEMBL175691 RILPIVIRINE 4.0 1 8.24
CHEMBL2012793 1 8.08
CHEMBL1632241 1 7.96
CHEMBL2165297 1 7.85
CHEMBL2165294 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165299 EC50 = 3.4 nM 8.47
CHEMBL2012795 EC50 = 3.4 nM 8.47
CHEMBL175691 RILPIVIRINE EC50 = 5.7 nM 8.24
CHEMBL2012793 EC50 = 8.3 nM 8.08
CHEMBL1632241 EC50 = 11.0 nM 7.96
CHEMBL2165297 EC50 = 14.0 nM 7.85
CHEMBL2165294 EC50 = 14.0 nM 7.85