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Assay Detail

CHEMBL4363880

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

Binding
Inhibition of NQO2 in human SKOV3 cells assessed as reduction in cell viability in presence of 1 uM CB1954 and EPR incubated for 24 hrs measured after 72 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ribosyldihydronicotinamide dehydrogenase [quinone] (CHEMBL3959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent 4-aminoquinoline hydrazone inhibitors of NRH:quinoneoxidoreductase-2 (NQO2).
Hussein B, Ikhmais B, Kadirvel M, Magwaza RN, Halbert G, Bryce RA, Stratford IJ, Freeman S.
Eur J Med Chem (2019) 182 : 111649 -111649
PubMed 31514018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.78 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436961 1 7.28
CHEMBL1967497 1 6.36
CHEMBL43184 AMINACRINE 2.0 1 6.35
CHEMBL4435240 1 6.01
CHEMBL4553527 1 5.68
CHEMBL4534563 1 4.64
CHEMBL4447586 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436961 IC50 = 53.0 nM 7.28
CHEMBL1967497 IC50 = 440.0 nM 6.36
CHEMBL43184 AMINACRINE IC50 = 450.0 nM 6.35
CHEMBL4435240 IC50 = 980.0 nM 6.01
CHEMBL4553527 IC50 = 2070.0 nM 5.68
CHEMBL4534563 IC50 = 22700.0 nM 4.64
CHEMBL4447586 IC50 = 74000.0 nM 4.13