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Assay Detail

CHEMBL3399803

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

Binding
Inhibition of CYP11B1 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 25 mins by HPLC analysis
19
Total Activities
19
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

Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
Grombein CM, Hu Q, Rau S, Zimmer C, Hartmann RW.
Eur J Med Chem (2015) 90 : 788 -796
PubMed 25528333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.70 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099695 OSILODROSTAT 4.0 1 8.54
CHEMBL3397607 1 8.35
CHEMBL9298 FADROZOLE 2.0 1 8.20
CHEMBL3397605 1 7.82
CHEMBL3397600 1 7.55
CHEMBL3397603 1 7.27
CHEMBL3397606 1 6.92
CHEMBL509971 1 6.28
CHEMBL3397599 1 6.11
CHEMBL3397602 1 6.10
CHEMBL3397597 1 5.88
CHEMBL3397604 1 5.77
CHEMBL3397601 1 5.46
CHEMBL62811 1 5.17
CHEMBL3397609 1 5.13
CHEMBL3397598 1 -
CHEMBL3397608 1 -
CHEMBL3397610 1 -
CHEMBL3397611 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099695 OSILODROSTAT IC50 = 2.9 nM 8.54
CHEMBL3397607 IC50 = 4.5 nM 8.35
CHEMBL9298 FADROZOLE IC50 = 6.3 nM 8.20
CHEMBL3397605 IC50 = 15.0 nM 7.82
CHEMBL3397600 IC50 = 28.0 nM 7.55
CHEMBL3397603 IC50 = 54.0 nM 7.27
CHEMBL3397606 IC50 = 120.0 nM 6.92
CHEMBL509971 IC50 = 525.0 nM 6.28
CHEMBL3397599 IC50 = 776.0 nM 6.11
CHEMBL3397602 IC50 = 796.0 nM 6.10
CHEMBL3397597 IC50 = 1312.0 nM 5.88
CHEMBL3397604 IC50 = 1692.0 nM 5.77
CHEMBL3397601 IC50 = 3451.0 nM 5.46
CHEMBL62811 IC50 = 6746.0 nM 5.17
CHEMBL3397609 IC50 = 7483.0 nM 5.13
CHEMBL3397598 IC50 - -
CHEMBL3397608 IC50 - -
CHEMBL3397610 IC50 - -
CHEMBL3397611 IC50 - -