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Assay Detail

CHEMBL3865969

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

Binding
Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days by Hoechst 33258 staining based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NAD(P)H dehydrogenase [quinone] 1 (CHEMBL3623)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and antitumor activity of selenium-containing quinone-based triazoles possessing two redox centres, and their mechanistic insights.
da Cruz EHG, Silvers MA, Jardim GAM, Resende JM, Cavalcanti BC, Bomfim IS, Pessoa C, de Simone CA, Botteselle GV, Braga AL, Nair DK, Namboothiri INN, Boothman DA, da Silva Júnior EN.
Eur J Med Chem (2016) 122 : 1 -16
PubMed 27341379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.77 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3939072 1 6.19
CHEMBL3966682 1 5.92
CHEMBL584338 1 5.89
CHEMBL516585 1 5.75
CHEMBL1098543 1 5.62
CHEMBL238792 1 5.58
CHEMBL15192 LAPACHONE 2.0 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3939072 IC50 = 640.0 nM 6.19
CHEMBL3966682 IC50 = 1200.0 nM 5.92
CHEMBL584338 IC50 = 1300.0 nM 5.89
CHEMBL516585 IC50 = 1800.0 nM 5.75
CHEMBL1098543 IC50 = 2400.0 nM 5.62
CHEMBL238792 IC50 = 2600.0 nM 5.58
CHEMBL15192 LAPACHONE IC50 = 3400.0 nM 5.47