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Assay Detail

CHEMBL5148482

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

Binding
Agonist activity at Gal4-fused human FXR in HEK293 cells incubated for 15 min by luciferase reporter assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bile acid receptor (CHEMBL2047)
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 33 6.96 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5181899 1 7.60
CHEMBL5202191 1 7.60
CHEMBL5187016 1 7.57
CHEMBL5170740 1 7.54
CHEMBL5182534 1 7.47
CHEMBL5177647 1 7.39
CHEMBL5189418 1 7.36
CHEMBL5190243 1 7.35
CHEMBL4862974 1 7.28
CHEMBL5169696 1 7.24
CHEMBL5174333 1 7.23
CHEMBL5190997 1 7.18
CHEMBL5172239 1 7.16
CHEMBL5174082 1 7.04
CHEMBL5180682 1 7.03
CHEMBL5178176 1 7.02
CHEMBL5182204 1 6.98
CHEMBL5173549 1 6.96
CHEMBL5203086 1 6.96
CHEMBL5199184 1 6.94
CHEMBL5184707 1 6.93
CHEMBL5196639 1 6.85
CHEMBL5184419 1 6.83
CHEMBL5205123 1 6.82
CHEMBL5178315 1 6.82
CHEMBL5189617 1 6.77
CHEMBL5194619 1 6.64
CHEMBL5208567 1 6.63
CHEMBL5191475 1 6.52
CHEMBL5204574 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5181899 EC50 = 25.0 nM 7.60
CHEMBL5202191 EC50 = 25.0 nM 7.60
CHEMBL5187016 EC50 = 27.0 nM 7.57
CHEMBL5170740 EC50 = 29.0 nM 7.54
CHEMBL5182534 EC50 = 34.0 nM 7.47
CHEMBL5177647 EC50 = 41.0 nM 7.39
CHEMBL5189418 EC50 = 44.0 nM 7.36
CHEMBL5190243 EC50 = 45.0 nM 7.35
CHEMBL4862974 EC50 = 53.0 nM 7.28
CHEMBL5169696 EC50 = 57.0 nM 7.24
CHEMBL5174333 EC50 = 59.0 nM 7.23
CHEMBL5190997 EC50 = 66.0 nM 7.18
CHEMBL5172239 EC50 = 70.0 nM 7.16
CHEMBL5174082 EC50 = 92.0 nM 7.04
CHEMBL5180682 EC50 = 93.0 nM 7.03
CHEMBL5178176 EC50 = 95.0 nM 7.02
CHEMBL5182204 EC50 = 104.0 nM 6.98
CHEMBL5173549 EC50 = 111.0 nM 6.96
CHEMBL5203086 EC50 = 111.0 nM 6.96
CHEMBL5199184 EC50 = 114.0 nM 6.94
CHEMBL5184707 EC50 = 118.0 nM 6.93
CHEMBL5196639 EC50 = 142.0 nM 6.85
CHEMBL5184419 EC50 = 149.0 nM 6.83
CHEMBL5205123 EC50 = 152.0 nM 6.82
CHEMBL5178315 EC50 = 152.0 nM 6.82
CHEMBL5189617 EC50 = 170.0 nM 6.77
CHEMBL5194619 EC50 = 228.0 nM 6.64
CHEMBL5208567 EC50 = 232.0 nM 6.63
CHEMBL5191475 EC50 = 299.0 nM 6.52
CHEMBL5204574 EC50 = 538.0 nM 6.27
CHEMBL5201654 EC50 = 919.0 nM 6.04
CHEMBL5204648 EC50 = 1092.0 nM 5.96
CHEMBL5205416 EC50 = 1638.0 nM 5.79