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Assay Detail

CHEMBL3784030

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

Binding
Inhibition of CYP17A1 in cynomolgus monkey using [3H]-pregnenolone as substrate incubated for 45 mins by scintillation proximity assay in presence of NADPH
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca fascicularis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3779754)
Type SINGLE PROTEIN
Organism Macaca fascicularis

Publication

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.
Huang A, Jayaraman L, Fura A, Vite GD, Trainor GL, Gottardis MM, Spires TE, Spires VM, Rizzo CA, Obermeier MT, Elzinga PA, Todderud G, Fan Y, Newitt JA, Beyer SM, Zhu Y, Warrack BM, Goodenough AK, Tebben AJ, Doweyko AM, Gold DL, Balog A.
ACS Med Chem Lett (2016) 7 : 40 -45
PubMed 26819663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.55 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3780847 1 8.70
CHEMBL2147041 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3780847 IC50 = 2.0 nM 8.70
CHEMBL2147041 IC50 = 4.0 nM 8.40