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Assay Detail

CHEMBL1177586

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Binding
Inhibition of human CYP11B2 expressed in hamster V79MZh cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79MZh
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B2, mitochondrial (CHEMBL2722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
Hu Q, Yin L, Jagusch C, Hille UE, Hartmann RW.
J Med Chem (2010) 53 : 5049 -5053
PubMed 20550118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.99 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 7.17
CHEMBL1173260 1 6.96
CHEMBL1172882 1 6.58
CHEMBL1173327 1 6.43
CHEMBL1171987 1 6.04
CHEMBL1172779 1 6.02
CHEMBL1172847 1 6.01
CHEMBL1171991 1 5.95
CHEMBL254328 ABIRATERONE 3.0 1 5.76
CHEMBL1173335 1 5.73
CHEMBL1173259 1 5.46
CHEMBL1173326 1 5.42
CHEMBL1172842 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 67.0 nM 7.17
CHEMBL1173260 IC50 = 110.0 nM 6.96
CHEMBL1172882 IC50 = 261.0 nM 6.58
CHEMBL1173327 IC50 = 368.0 nM 6.43
CHEMBL1171987 IC50 = 921.0 nM 6.04
CHEMBL1172779 IC50 = 948.0 nM 6.02
CHEMBL1172847 IC50 = 974.0 nM 6.01
CHEMBL1171991 IC50 = 1130.0 nM 5.95
CHEMBL254328 ABIRATERONE IC50 = 1750.0 nM 5.76
CHEMBL1173335 IC50 = 1870.0 nM 5.73
CHEMBL1173259 IC50 = 3450.0 nM 5.46
CHEMBL1173326 IC50 = 3830.0 nM 5.42
CHEMBL1172842 IC50 = 49500.0 nM 4.30