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Assay Detail

CHEMBL3750856

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

Binding
Inhibition human recombinant CYP11B1 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay
1
Total Activities
1
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

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

Publication

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C.
J Med Chem (2015) 58 : 9382 -9394
PubMed 26540564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.60 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099695 OSILODROSTAT 4.0 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099695 OSILODROSTAT IC50 = 2.5 nM 8.60