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Assay Detail

CHEMBL2169293

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

Binding
Inhibition of human CYP17 expressed in Escherichia coli using progesterone substrate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome.
Yin L, Lucas S, Maurer F, Kazmaier U, Hu Q, Hartmann RW.
J Med Chem (2012) 55 : 6629 -6633
PubMed 22788843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.16 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254328 ABIRATERONE 3.0 1 7.14
CHEMBL2163638 1 5.81
CHEMBL2163639 1 5.54
CHEMBL2163646 1 -
CHEMBL2163641 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254328 ABIRATERONE IC50 = 72.0 nM 7.14
CHEMBL2163638 IC50 = 1550.0 nM 5.81
CHEMBL2163639 IC50 = 2880.0 nM 5.54
CHEMBL2163646 IC50 > 5000.0 nM -
CHEMBL2163641 IC50 > 5000.0 nM -