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Assay Detail

CHEMBL866708

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

Binding
Inhibition of rat microsomal 17-alpha-hydroxylase component of P450-17alpha
16
Total Activities
16
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 and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)).
Owen CP, Dhanani S, Patel CH, Shahid I, Ahmed S.
Bioorg Med Chem Lett (2006) 16 : 4011 -4015
PubMed 16750362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.50 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 5.42
CHEMBL427399 1 5.00
CHEMBL379436 1 4.91
CHEMBL210125 1 4.65
CHEMBL13784 1 4.60
CHEMBL211276 1 4.59
CHEMBL441367 1 4.50
CHEMBL349822 1 4.39
CHEMBL212741 1 4.30
CHEMBL211207 1 4.27
CHEMBL373588 1 4.15
CHEMBL166845 1 4.14
CHEMBL446946 1 4.08
CHEMBL377770 1 4.06
CHEMBL213596 1 -
CHEMBL14192 BENZYLIMIDAZOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 3760.0 nM 5.42
CHEMBL427399 IC50 = 10060.0 nM 5.00
CHEMBL379436 IC50 = 12220.0 nM 4.91
CHEMBL210125 IC50 = 22560.0 nM 4.65
CHEMBL13784 IC50 = 25380.0 nM 4.60
CHEMBL211276 IC50 = 25950.0 nM 4.59
CHEMBL441367 IC50 = 31630.0 nM 4.50
CHEMBL349822 IC50 = 40260.0 nM 4.39
CHEMBL212741 IC50 = 50560.0 nM 4.30
CHEMBL211207 IC50 = 53400.0 nM 4.27
CHEMBL373588 IC50 = 70660.0 nM 4.15
CHEMBL166845 IC50 = 72050.0 nM 4.14
CHEMBL446946 IC50 = 83100.0 nM 4.08
CHEMBL377770 IC50 = 86580.0 nM 4.06
CHEMBL213596 IC50 = 244850.0 nM -
CHEMBL14192 BENZYLIMIDAZOLE IC50 = 214580.0 nM -