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Assay Detail

CHEMBL892390

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

Binding
Inhibition of FXR in HEK293 cells in presence of CDCA by GAL4 transactivation activity
6
Total Activities
6
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 Intermediate

Target

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

Publication

Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
Kainuma M, Makishima M, Hashimoto Y, Miyachi H.
Bioorg Med Chem (2007) 15 : 2587 -2600
PubMed 17292610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.95 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234747 1 5.43
CHEMBL234371 1 5.40
CHEMBL410683 GUGGULSTERONE 1 4.92
CHEMBL274652 1 4.80
CHEMBL231899 1 4.65
CHEMBL398012 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234747 IC50 = 3700.0 nM 5.43
CHEMBL234371 IC50 = 4000.0 nM 5.40
CHEMBL410683 GUGGULSTERONE IC50 = 12000.0 nM 4.92
CHEMBL274652 IC50 = 15800.0 nM 4.80
CHEMBL231899 IC50 = 22200.0 nM 4.65
CHEMBL398012 IC50 = 33900.0 nM 4.47