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Assay Detail

CHEMBL1004505

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Binding
Binding affinity to human recombinant carbonyl reductase 1 expressed in Escherichia coli assessed as NADPH oxidation using isatin as substrate
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonyl reductase [NADPH] 1 (CHEMBL5586)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone.
Zimmermann TJ, Niesen FH, Pilka ES, Knapp S, Oppermann U, Maier ME.
Bioorg Med Chem (2009) 17 : 530 -536
PubMed 19097799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.68 6.68
Ki 7 6.46 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453375 2 7.40
CHEMBL849 TRICLOSAN 4.0 2 7.22
CHEMBL117 CHRYSIN 2 6.96
CHEMBL414883 RADICICOL 2 6.28
CHEMBL97453 WEDELOLACTONE 2 6.22
CHEMBL131921 BIOCHANIN 2 5.69
CHEMBL9352 NARINGENIN 2 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453375 Ki = 40.0 nM 7.40
CHEMBL849 TRICLOSAN Ki = 60.0 nM 7.22
CHEMBL117 CHRYSIN Ki = 110.0 nM 6.96
CHEMBL453375 IC50 = 210.0 nM 6.68
CHEMBL849 TRICLOSAN IC50 = 400.0 nM 6.40
CHEMBL414883 RADICICOL Ki = 520.0 nM 6.28
CHEMBL97453 WEDELOLACTONE Ki = 600.0 nM 6.22
CHEMBL117 CHRYSIN IC50 = 670.0 nM 6.17
CHEMBL131921 BIOCHANIN Ki = 2030.0 nM 5.69
CHEMBL414883 RADICICOL IC50 = 3270.0 nM 5.49
CHEMBL9352 NARINGENIN Ki = 3430.0 nM 5.46
CHEMBL97453 WEDELOLACTONE IC50 = 3780.0 nM 5.42
CHEMBL131921 BIOCHANIN IC50 = 12710.0 nM 4.90
CHEMBL9352 NARINGENIN IC50 = 21480.0 nM 4.67