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Assay Detail

CHEMBL1041085

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

Functional
Antiviral activity against HIV1 RTMDR1 infected in human TZM-bl cells assessed as inhibition of viral replication
15
Total Activities
15
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

Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Tian X, Qin B, Lu H, Lai W, Jiang S, Lee KH, Chen CH, Xie L.
Bioorg Med Chem Lett (2009) 19 : 5482 -5485
PubMed 19666220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.49 9.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70663 DAPIVIRINE 3.0 1 9.53
CHEMBL569259 1 9.02
CHEMBL566806 1 8.92
CHEMBL566153 1 8.42
CHEMBL569258 1 8.29
CHEMBL569051 1 8.04
CHEMBL569520 1 7.68
CHEMBL577081 1 7.60
CHEMBL567462 1 7.26
CHEMBL569494 1 7.03
CHEMBL565323 1 6.89
CHEMBL566152 1 6.67
CHEMBL566594 1 6.28
CHEMBL585572 1 6.06
CHEMBL568535 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70663 DAPIVIRINE EC50 = 0.298 nM 9.53
CHEMBL569259 EC50 = 0.96 nM 9.02
CHEMBL566806 EC50 = 1.2 nM 8.92
CHEMBL566153 EC50 = 3.78 nM 8.42
CHEMBL569258 EC50 = 5.13 nM 8.29
CHEMBL569051 EC50 = 9.03 nM 8.04
CHEMBL569520 EC50 = 21.1 nM 7.68
CHEMBL577081 EC50 = 25.1 nM 7.60
CHEMBL567462 EC50 = 55.2 nM 7.26
CHEMBL569494 EC50 = 94.3 nM 7.03
CHEMBL565323 EC50 = 128.0 nM 6.89
CHEMBL566152 EC50 = 215.0 nM 6.67
CHEMBL566594 EC50 = 531.0 nM 6.28
CHEMBL585572 EC50 = 877.0 nM 6.06
CHEMBL568535 EC50 = 25480.0 nM 4.59