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Assay Detail

CHEMBL662845

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Binding
Inhibition of rat testicular microsomal Cytochrome P450 17A1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL4430)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha).
Ling YZ, Li JS, Liu Y, Kato K, Klus GT, Brodie A.
J Med Chem (1997) 40 : 3297 -3304
PubMed 9379450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.83 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325307 1 7.85
CHEMBL2112517 1 7.55
CHEMBL78215 1 7.50
CHEMBL2112526 1 7.31
CHEMBL113448 1 7.12
CHEMBL113966 1 7.10
CHEMBL2112521 1 7.08
CHEMBL2112518 1 7.04
CHEMBL157101 KETOCONAZOLE 4.0 1 5.97
CHEMBL2112533 1 5.32
CHEMBL2112524 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325307 IC50 = 14.0 nM 7.85
CHEMBL2112517 IC50 = 28.0 nM 7.55
CHEMBL78215 IC50 = 32.0 nM 7.50
CHEMBL2112526 IC50 = 49.0 nM 7.31
CHEMBL113448 IC50 = 76.0 nM 7.12
CHEMBL113966 IC50 = 79.0 nM 7.10
CHEMBL2112521 IC50 = 84.0 nM 7.08
CHEMBL2112518 IC50 = 91.0 nM 7.04
CHEMBL157101 KETOCONAZOLE IC50 = 1067.0 nM 5.97
CHEMBL2112533 IC50 = 4813.0 nM 5.32
CHEMBL2112524 IC50 = 5456.0 nM 5.26