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Assay Detail

CHEMBL908004

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

Binding
Inhibition of rat testis 17-alpha-hydroxylase component of P450-17alpha
13
Total Activities
13
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

Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)).
Patel CH, Dhanani S, Owen CP, Ahmed S.
Bioorg Med Chem Lett (2006) 16 : 4752 -4756
PubMed 16870430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.74 5.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386256 1 5.53
CHEMBL157101 KETOCONAZOLE 4.0 1 5.42
CHEMBL213493 1 5.23
CHEMBL211207 1 4.78
CHEMBL214932 1 4.56
CHEMBL441367 1 4.53
CHEMBL215320 1 4.51
CHEMBL380271 1 4.51
CHEMBL379290 1 4.30
CHEMBL377770 1 4.02
CHEMBL14192 BENZYLIMIDAZOLE 1 -
CHEMBL215425 1 -
CHEMBL385589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386256 IC50 = 2950.0 nM 5.53
CHEMBL157101 KETOCONAZOLE IC50 = 3760.0 nM 5.42
CHEMBL213493 IC50 = 5850.0 nM 5.23
CHEMBL211207 IC50 = 16550.0 nM 4.78
CHEMBL214932 IC50 = 27810.0 nM 4.56
CHEMBL441367 IC50 = 29840.0 nM 4.53
CHEMBL215320 IC50 = 30660.0 nM 4.51
CHEMBL380271 IC50 = 30950.0 nM 4.51
CHEMBL379290 IC50 = 49640.0 nM 4.30
CHEMBL377770 IC50 = 96460.0 nM 4.02
CHEMBL14192 BENZYLIMIDAZOLE IC50 = 154200.0 nM -
CHEMBL215425 IC50 = 120200.0 nM -
CHEMBL385589 IC50 - -