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Assay Detail

CHEMBL3750827

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Functional
Decrease in ACTH-stimulated plasma aldosterone level in po dosed chair-trained chronically cannulated cynomolgus monkey model compound administered followed by ACTH challenge for 3 hrs measured after 24 hrs by LC/MS/MS analysis
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Macaca fascicularis
Tissue Plasma
Confidence 1 — Organism
Curated By Autocuration

Target

Cynomolgus monkey (CHEMBL613847)
Type ORGANISM
Organism Macaca fascicularis

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
Activity 1 - -
ED50 1 - -
EC50 1 8.07 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747562 3 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747562 EC50 = 8.5 nM 8.07
CHEMBL3747562 Activity - -
CHEMBL3747562 ED50 = 0.061 mg.kg-1 -