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Approval Year

Substance Class Protein
Created
by admin
on Tue Apr 01 17:44:15 GMT 2025
Edited
by admin
on Tue Apr 01 17:44:15 GMT 2025
Protein Type RECEPTOR
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
0C5V0MRU6P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BILE ACID RECEPTOR
Common Name English
BILE ACID RECEPTOR (HUMAN)
Preferred Name English
FARNESOID X-ACTIVATED RECEPTOR
Common Name English
RXR-INTERACTING PROTEIN 14
Common Name English
RETINOID X RECEPTOR-INTERACTING PROTEIN 14
Common Name English
FXR (HUMAN)
Common Name English
FARNESOID X RECEPTOR
Common Name English
NUCLEAR RECEPTOR SUBFAMILY 1 GROUP H MEMBER 4
Systematic Name English
NR1H4
Common Name English
FXR
Common Name English
Code System Code Type Description
FDA UNII
0C5V0MRU6P
Created by admin on Tue Apr 01 17:44:15 GMT 2025 , Edited by admin on Tue Apr 01 17:44:15 GMT 2025
PRIMARY
Related Record Type Details
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
When bound to bile acids, FXR repressed transcription of the gene encoding cholesterol 7α-hydroxylase, which is the rate-limiting enzyme in bile acid synthesis, and activated the gene encoding intestinal bile acid?binding protein, which is a candidate bile acid transporter.
AGONIST
AGONIST -> TARGET
Alpha screen
AGONIST -> TARGET
AGONIST -> TARGET
Time-resolved fluorescence resonance energy (TR-FRET)
BINDING
EC50
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR->OFF-TARGET
Inhibition of the FXR by danicopan has the potential to promote cholestasis.
AGONIST -> TARGET
GAL-4 ASSAY
AGONIST -> TARGET
CDCA, had a half-maximal effective concentration (EC50) of 50 mMand 10 micromolar murine and human FXR, respectively (Fig. 1B). These concentrations are well within the physiologic intracellular range reported in vivo (11).
AGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
IC50
AGONIST -> TARGET

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID REPLACEMENT [1_145] [1_164] SERINE DEXFOSFOSERINE VI4F0K069V
AMINO ACID REPLACEMENT [1_456] THREONINE THREONINE PHOSPHATE 3L4WX7B1EI
AMINO ACID REPLACEMENT [1_167] [1_227] LYSINE N6-ACETYLLYSINE 470AD5VY1X
AMINO ACID REPLACEMENT [1_220] LYSINE N6-METHYLLYSINE FCR6T2IYVU
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) CHEMICAL