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Assay Detail

CHEMBL3537682

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ADMET
Uncompetitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as enzyme-substrate complex by Lineweaver-Burk plot analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldehyde oxidase (CHEMBL3257)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase.
Barr JT, Jones JP.
Drug Metab Dispos (2013) 41 : 24 -29
PubMed 22996261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.54 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL590 MENADIONE 4.0 1 5.82
CHEMBL691 ETHINYL ESTRADIOL 4.0 1 5.44
CHEMBL135 ESTRADIOL 4.0 1 5.36
CHEMBL42 CLOZAPINE 4.0 1 -
CHEMBL81 RALOXIFENE 4.0 1 -
CHEMBL71 CHLORPROMAZINE 4.0 1 -
CHEMBL219916 DOMPERIDONE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL590 MENADIONE Ki = 1500.0 nM 5.82
CHEMBL691 ETHINYL ESTRADIOL Ki = 3600.0 nM 5.44
CHEMBL135 ESTRADIOL Ki = 4400.0 nM 5.36
CHEMBL42 CLOZAPINE Ki - -
CHEMBL81 RALOXIFENE Ki - -
CHEMBL71 CHLORPROMAZINE Ki - -
CHEMBL219916 DOMPERIDONE Ki - -