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Assay Detail

CHEMBL3366443

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

Binding
Inhibition of human CYP11B1 expressed in V79 MZ cells pretreated with compound for 1 hr followed by addition of 500 nM 11-deoxycorticosterone for 3 hrs by HPLC analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79MZ
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B1, mitochondrial (CHEMBL1908)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
Hu Q, Yin L, Hartmann RW.
J Med Chem (2014) 57 : 5011 -5022
PubMed 24422519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.58 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL681 ETOMIDATE 4.0 1 9.30
CHEMBL934 METYRAPONE 4.0 1 7.34
CHEMBL287677 DEXFADROSTAT 2.0 1 6.92
CHEMBL31215 S-FADROZOLE 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL681 ETOMIDATE IC50 = 0.5 nM 9.30
CHEMBL934 METYRAPONE IC50 = 46.0 nM 7.34
CHEMBL287677 DEXFADROSTAT IC50 = 119.0 nM 6.92
CHEMBL31215 S-FADROZOLE IC50 = 171.0 nM 6.77