Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5148484

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

Binding
Agonist activity at mouse LBD fused FXR in HEK293 cells incubated for 30 min by envision plate reader method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bile acid receptor (CHEMBL5343)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Nara SJ, Jogi S, Cheruku S, Kandhasamy S, Jaipuri F, Kathi PK, Reddy S, Sarodaya S, Cook EM, Wang T, Sitkoff D, Rossi KA, Ruzanov M, Kiefer SE, Khan JA, Gao M, Reddy S, Sivaprasad Lvj S, Sane R, Mosure K, Zhuo X, Cao GG, Ziegler M, Azzara A, Krupinski J, Soars MG, Ellsworth BA, Wacker DA.
J Med Chem (2022) 65 : 8948 -8960
PubMed 35704802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.18 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5182534 1 7.85
CHEMBL4862974 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5182534 EC50 = 14.0 nM 7.85
CHEMBL4862974 EC50 = 320.0 nM 6.50