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Assay Detail

CHEMBL1228229

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Binding
Inhibition of 17,20-lyase activity of rat testicular microsomal P450-17alpha
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes.
Owen CP, Shahid I, Lee WY, Ahmed S.
Bioorg Med Chem Lett (2010) 20 : 5345 -5348
PubMed 20675132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.23 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1222987 1 8.00
CHEMBL560398 1 7.85
CHEMBL1222850 1 7.70
CHEMBL539453 1 7.52
CHEMBL1222922 1 7.52
CHEMBL560333 1 7.47
CHEMBL1222923 1 7.40
CHEMBL1222924 1 6.80
CHEMBL427399 1 6.79
CHEMBL157101 KETOCONAZOLE 4.0 1 6.69
CHEMBL166845 1 5.83
CHEMBL14192 BENZYLIMIDAZOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1222987 IC50 = 10.0 nM 8.00
CHEMBL560398 IC50 = 14.0 nM 7.85
CHEMBL1222850 IC50 = 20.0 nM 7.70
CHEMBL539453 IC50 = 30.0 nM 7.52
CHEMBL1222922 IC50 = 30.0 nM 7.52
CHEMBL560333 IC50 = 34.0 nM 7.47
CHEMBL1222923 IC50 = 40.0 nM 7.40
CHEMBL1222924 IC50 = 160.0 nM 6.80
CHEMBL427399 IC50 = 164.0 nM 6.79
CHEMBL157101 KETOCONAZOLE IC50 = 206.0 nM 6.69
CHEMBL166845 IC50 = 1470.0 nM 5.83
CHEMBL14192 BENZYLIMIDAZOLE IC50 > 3000.0 nM -