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Assay Detail

CHEMBL5148485

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

Binding
Agonist activity at human FXR2 expressed in Huh-7 cells coexpressing BSEP relative to GW2064
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Huh-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

RNA-binding protein FXR2 (CHEMBL5169136)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.55 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862974 1 6.55
CHEMBL5182534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862974 EC50 = 281.0 nM 6.55
CHEMBL5182534 EC50 > 40000.0 nM -