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Assay Detail

CHEMBL4016417

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

Functional
In vivo inhibition of 11beta-HSD1 in po dosed non-fasting diet-induced obese mouse assessed as plasma concentration required to show decrease in corticosterone excursion pretreated for 60 mins followed by DHC administration measured up to 120 mins by enzyme immunosorbent assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Ye XY, Chen SY, Wu S, Yoon DS, Wang H, Hong Z, O'Connor SP, Li J, Li JJ, Kennedy LJ, Walker SJ, Nayeem A, Sheriff S, Camac DM, Ramamurthy V, Morin PE, Zebo R, Taylor JR, Morgan NN, Ponticiello RP, Harrity T, Apedo A, Golla R, Seethala R, Wang M, Harper TW, Sleczka BG, He B, Kirby M, Leahy DK, Li J, Hanson RL, Guo Z, Li YX, DiMarco JD, Scaringe R, Maxwell B, Moulin F, Barrish JC, Gordon DA, Robl JA.
J Med Chem (2017) 60 : 4932 -4948
PubMed 28537398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.07 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080667 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080667 EC50 = 850.0 nM 6.07