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Assay Detail

CHEMBL656739

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

Functional
Concentration which produces a 50% survival of HIV-1 infected cells relative to uninfected control C8166 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type C8166
Confidence 1 — Organism
Curated By Expert

Target

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

Publication

Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Campiani G, Aiello F, Fabbrini M, Morelli E, Ramunno A, Armaroli S, Nacci V, Garofalo A, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Ventura L, Bongiovanni B, Capozzi M, Bolacchi F, Marini S, Coletta M, Guiso G, Caccia S.
J Med Chem (2001) 44 : 305 -315
PubMed 11462972 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.10 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418833 1 7.70
CHEMBL105916 1 7.60
CHEMBL105976 1 7.60
CHEMBL58711 TIVIRAPINE 2.0 1 7.52
CHEMBL418812 1 7.50
CHEMBL110091 1 7.21
CHEMBL107535 1 6.91
CHEMBL107099 1 6.70
CHEMBL320557 1 6.50
CHEMBL108221 1 6.42
CHEMBL129 ZIDOVUDINE 4.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418833 EC50 = 20.0 nM 7.70
CHEMBL105916 EC50 = 25.0 nM 7.60
CHEMBL105976 EC50 = 25.0 nM 7.60
CHEMBL58711 TIVIRAPINE EC50 = 30.0 nM 7.52
CHEMBL418812 EC50 = 32.0 nM 7.50
CHEMBL110091 EC50 = 61.0 nM 7.21
CHEMBL107535 EC50 = 124.0 nM 6.91
CHEMBL107099 EC50 = 200.0 nM 6.70
CHEMBL320557 EC50 = 320.0 nM 6.50
CHEMBL108221 EC50 = 380.0 nM 6.42
CHEMBL129 ZIDOVUDINE EC50 = 400.0 nM 6.40