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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL2047
Target Type SINGLE PROTEIN
Preferred Name Bile acid receptor FXR
Synonyms BAR | Bile acid receptor | FXR | Farnesoid X-activated receptor | Farnesol receptor HRR-1 | HRR1 | NR1H4 | Nuclear receptor subfamily 1 group H member 4 | RIP14 | RXR-interacting protein 14 | Retinoid X receptor-interacting protein 14
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor > nuclear receptor > nuclear hormone receptor subfamily 1 > nuclear hormone receptor subfamily 1 group h > nuclear hormone receptor subfamily 1 group h member 4

Target Components

Component Description Relationship Accession
Bile acid receptor SINGLE PROTEIN Q96RI1

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL240597 CHENODIOL Bile acid receptor FXR agonist 4 DailyMed PubMed
CHEMBL1551 URSODIOL Bile acid receptor FXR agonist 4 PubMed PubMed PubMed
CHEMBL566315 OBETICHOLIC ACID Bile acid receptor FXR agonist 4 Other PubMed
CHEMBL454138 TUROFEXORATE ISOPROPYL Bile acid receptor FXR agonist 1 PubMed PubMed
CHEMBL3545113 Px-102 Bile acid receptor FXR agonist 1 Other Other PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000012504
Ensembl ENSG00000012504
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005719 (nuclear euchromatin)
GO Molecular Function GO:0000980 (RNA polymerase II distal enhancer sequence-specific DNA binding)
GO:0001077 (transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001190 (transcriptional activator activity, RNA polymerase II transcription factor binding)
GO:0003677 (DNA binding)
GO:0003690 (double-stranded DNA binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003705 (transcription factor activity, RNA polymerase II distal enhancer sequence-specific binding)
GO:0003707 (steroid hormone receptor activity)
GO:0003713 (transcription coactivator activity)
GO:0003714 (transcription corepressor activity)
GO:0004872 (receptor activity)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0004887 (thyroid hormone receptor activity)
GO:0005515 (protein binding)
GO:0008270 (zinc ion binding)
GO:0016922 (ligand-dependent nuclear receptor binding)
GO:0032052 (bile acid binding)
GO:0038181 (bile acid receptor activity)
GO:0042277 (peptide binding)
GO:0043565 (sequence-specific DNA binding)
GO:0046872 (metal ion binding)
GO:0046965 (retinoid X receptor binding)
GO:1902122 (chenodeoxycholic acid binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001080 (nitrogen catabolite activation of transcription from RNA polymerase II promoter)
GO:0002376 (immune system process)
GO:0006109 (regulation of carbohydrate metabolic process)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006357 (regulation of transcription from RNA polymerase II promoter)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007219 (Notch signaling pathway)
GO:0008206 (bile acid metabolic process)
GO:0009749 (response to glucose)
GO:0010988 (regulation of low-density lipoprotein particle clearance)
GO:0015721 (bile acid and bile salt transport)
GO:0030522 (intracellular receptor signaling pathway)
GO:0032496 (response to lipopolysaccharide)
GO:0034142 (toll-like receptor 4 signaling pathway)
GO:0034255 (regulation of urea metabolic process)
GO:0034971 (histone H3-R17 methylation)
GO:0035356 (cellular triglyceride homeostasis)
GO:0038183 (bile acid signaling pathway)
GO:0038185 (intracellular bile acid receptor signaling pathway)
GO:0043066 (negative regulation of apoptotic process)
GO:0043124 (negative regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0045087 (innate immune response)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048565 (digestive tract development)
GO:0061178 (regulation of insulin secretion involved in cellular response to glucose stimulus)
GO:0070857 (regulation of bile acid biosynthetic process)
GO:0070858 (negative regulation of bile acid biosynthetic process)
GO:0071398 (cellular response to fatty acid)
GO:0071417 (cellular response to organonitrogen compound)
GO:0072615 (interleukin-17 secretion)
GO:0090181 (regulation of cholesterol metabolic process)
GO:1902714 (negative regulation of interferon-gamma secretion)
GO:1904468 (negative regulation of tumor necrosis factor secretion)
GO:2000213 (positive regulation of glutamate metabolic process)
GO:2001250 (positive regulation of ammonia assimilation cycle)
Wikipedia Farnesoid_X_receptor

Target Cross References - Protein

canSAR Q96RI1
Human Protein Atlas ENSG00000012504
IntAct Q96RI1
Guide to Pharmacology 603
Open Targets ENSG00000012504
PharmGKB PA31752
Pharos Q96RI1 (Tclin)
Reactome R-HSA-159418 (Recycling of bile acids and salts.)
R-HSA-192105 (Synthesis of bile acids and bile salts.)
R-HSA-193368 (Synthesis of bile acids and bile salts via 7alpha-hydroxycholesterol.)
R-HSA-193807 (Synthesis of bile acids and bile salts via 27-hydroxycholesterol.)
R-HSA-1989781 (PPARA activates gene expression.)
R-HSA-211976 (Endogenous sterols.)
R-HSA-383280 (Nuclear Receptor transcription pathway.)
UniProt A1L4K5 B7Z412 B7ZM06 F8VYG8 Q8NFP5 Q8NFP6 Q92943 Q96RI1

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR001628 (Znf_hrmn_rcpt.)
IPR001723 (Nuclear_hrmn_rcpt.)
IPR001728 (ThyrH_rcpt.)
IPR013088 (Znf_NHR/GATA.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)

Target Cross References - Structure

PDBe 1OSH 3BEJ 3DCT 3DCU 3FLI 3FXV 3GD2 3HC5 3HC6 3L1B 3OKH 3OKI 3OLF 3OMK 3OMM 3OOF 3OOK 3P88 3P89 3RUT 3RUU 3RVF 4OIV 4QE6 More...
CREDO 1OSH 3BEJ 3DCT 3DCU 3FLI 3FXV 3GD2 3HC5 3HC6 3L1B 3OKH 3OKI 3OLF 3OMK 3OMM 3OOF 3OOK 3P88 3P89 3RUT 3RUU 3RVF 4OIV 4QE6 More...
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