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Assay Detail

CHEMBL5236198

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

Binding
Agonist activity at FXR in human HeLa cells incubated for 24 hrs by Dual-Glo luciferase assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bile acid receptor (CHEMBL2047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor.
Fang Y, Hegazy L, Finck BN, Elgendy B.
J Med Chem (2021) 64 : 17545 -17571
PubMed 34889100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.95 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5272705 1 6.64
CHEMBL5281274 1 6.58
CHEMBL5272000 1 6.52
CHEMBL4632533 1 6.10
CHEMBL5273108 1 5.46
CHEMBL603 ZAFIRLUKAST 4.0 1 5.41
CHEMBL5283234 1 4.96
CHEMBL4633499 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5272705 EC50 = 230.0 nM 6.64
CHEMBL5281274 EC50 = 260.0 nM 6.58
CHEMBL5272000 EC50 = 300.0 nM 6.52
CHEMBL4632533 EC50 = 800.0 nM 6.10
CHEMBL5273108 EC50 = 3500.0 nM 5.46
CHEMBL603 ZAFIRLUKAST EC50 = 3900.0 nM 5.41
CHEMBL5283234 EC50 = 11000.0 nM 4.96
CHEMBL4633499 EC50 = 940000.0 nM -