Page last updated: 2024-08-07 18:48:03
Bile acid receptor
A bile acid receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96RI1]
Synonyms
Farnesoid X-activated receptor;
Farnesol receptor HRR-1;
Nuclear receptor subfamily 1 group H member 4;
Retinoid X receptor-interacting protein 14;
RXR-interacting protein 14
Research
Bioassay Publications (81)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 25 (30.86) | 29.6817 |
2010's | 44 (54.32) | 24.3611 |
2020's | 12 (14.81) | 2.80 |
Compounds (44)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
clotrimazole | Homo sapiens (human) | IC50 | 3.2400 | 1 | 1 |
felodipine | Homo sapiens (human) | IC50 | 4.9600 | 1 | 1 |
flutrimazole | Homo sapiens (human) | IC50 | 13.8000 | 1 | 1 |
loratadine | Homo sapiens (human) | IC50 | 3.0700 | 1 | 1 |
nimodipine | Homo sapiens (human) | IC50 | 8.9600 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 11.5600 | 1 | 1 |
sulconazole | Homo sapiens (human) | IC50 | 6.8800 | 1 | 1 |
thyroxine | Homo sapiens (human) | IC50 | 7.8600 | 1 | 1 |
lithocholic acid | Homo sapiens (human) | IC50 | 0.0183 | 1 | 1 |
fulvestrant | Homo sapiens (human) | IC50 | 0.7900 | 1 | 1 |
6-hydroxydopa | Homo sapiens (human) | IC50 | 7.9200 | 1 | 1 |
ly 255283 | Homo sapiens (human) | IC50 | 35.2000 | 1 | 1 |
nbi 27914 | Homo sapiens (human) | IC50 | 2.7700 | 1 | 1 |
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol | Homo sapiens (human) | IC50 | 1.3100 | 1 | 1 |
t0901317 | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 3.4000 | 1 | 1 |
gw 7647 | Homo sapiens (human) | IC50 | 4.9100 | 1 | 1 |
jhw 015 | Homo sapiens (human) | IC50 | 3.2200 | 1 | 1 |
andrographolide | Homo sapiens (human) | IC50 | 9.7000 | 2 | 2 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 27.4778 | 9 | 9 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | IC50 | 51.0943 | 7 | 7 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
gw 4064 | Homo sapiens (human) | IC50 | 0.0650 | 4 | 4 |
12-epi-scalarin | Homo sapiens (human) | IC50 | 60.4000 | 1 | 1 |
glycoursodeoxycholic acid | Homo sapiens (human) | IC50 | 98.4000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
gw 4064 | Homo sapiens (human) | Activity | 0.0640 | 1 | 1 |
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor.Bioorganic & medicinal chemistry, , Jun-01, Volume: 22, Issue:11, 2014
Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking.MedChemComm, , Oct-01, Volume: 9, Issue:10, 2018
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Novel FXR (farnesoid X receptor) modulators: Potential therapies for cholesterol gallstone disease.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Novel approaches to map small molecule-target interactions.Bioorganic & medicinal chemistry, , Aug-01, Volume: 24, Issue:15, 2016
Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Pharmacophore-based discovery of FXR-agonists. Part II: identification of bioactive triterpenes from Ganoderma lucidum.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation.Proceedings of the National Academy of Sciences of the United States of America, , Apr-08, Volume: 105, Issue:14, 2008
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Farnesoid X receptor: from structure to potential clinical applications.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.Journal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Identification of a chemical tool for the orphan nuclear receptor FXR.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Farnesoid X receptor: from structure to potential clinical applications.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.Journal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
A novel intestinal-restricted FXR agonist.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Discovery of new non-steroidal FXR ligands via a virtual screening workflow based on Phase shape and induced fit docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Diversity-oriented synthesis: exploring the intersections between chemistry and biology.Nature chemical biology, , Volume: 1, Issue:2, 2005
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
The Halicylindramides, Farnesoid X Receptor Antagonizing Depsipeptides from a Petrosia sp. Marine Sponge Collected in Korea.Journal of natural products, , Mar-25, Volume: 79, Issue:3, 2016
Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus.Journal of natural products, , Jan-28, Volume: 74, Issue:1, 2011
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.Journal of natural products, , Volume: 70, Issue:11, 2007
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists.Bioorganic & medicinal chemistry, , 03-15, Volume: 25, Issue:6, 2017
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 22, Issue:5, 2014
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 16, Issue:20, 2006
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Design, synthesis and biological evaluations of novel farnesoid X receptor (FXR) agonists.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Design, synthesis, and biological studies of novel 3-benzamidobenzoic acid derivatives as farnesoid X receptor partial agonist.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design and Structural Optimization of Dual FXR/PPARδ Activators.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
[no title available]Bioorganic & medicinal chemistry, , 07-15, Volume: 28, Issue:14, 2020
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 25, Issue:2, 2015
Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor.Bioorganic & medicinal chemistry, , Jun-01, Volume: 22, Issue:11, 2014
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR).Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
Discovery of new non-steroidal FXR ligands via a virtual screening workflow based on Phase shape and induced fit docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
FXR agonist activity of conformationally constrained analogs of GW 4064.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 18, Issue:15, 2008
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Farnesoid X receptor: from structure to potential clinical applications.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.Journal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Identification of a chemical tool for the orphan nuclear receptor FXR.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR).Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 19, Issue:18, 2009
Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR).Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Enables
This protein enables 15 target(s):
Target | Category | Definition |
RNA polymerase II transcription regulatory region sequence-specific DNA binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls the transcription of a gene or cistron by RNA polymerase II. [GOC:txnOH] |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
transcription coregulator binding | molecular function | Binding to a transcription coregulator, a protein involved in regulation of transcription via protein-protein interactions with transcription factors and other transcription regulatory proteins. Cofactors do not bind DNA directly, but rather mediate protein-protein interactions between regulatory transcription factors and the basal transcription machinery. [GOC:krc] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
nuclear receptor binding | molecular function | Binding to a nuclear receptor protein. Nuclear receptor proteins are DNA-binding transcription factors which are regulated by binding to a ligand. [PMID:7776974] |
bile acid binding | molecular function | Binding to a bile acid, a steroid carboxylic acids occurring in bile. [GOC:rph] |
bile acid receptor activity | molecular function | Combining with a bile acid and transmitting the signal to initiate a change in cell activity. A bile acid is any member of a group of steroid carboxylic acids occurring in bile. [GOC:bf, PMID:10334992, PMID:12718893] |
sequence-specific DNA binding | molecular function | Binding to DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA e.g. promotor binding or rDNA binding. [GOC:jl] |
nuclear retinoid X receptor binding | molecular function | Binding to a nuclear retinoid X receptor. [GOC:ai] |
chenodeoxycholic acid binding | molecular function | Binding to chenodeoxycholic acid. [GOC:bf, GOC:TermGenie, PMID:10334992] |
Located In
This protein is located in 1 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 4 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
euchromatin | cellular component | A dispersed and relatively uncompacted form of chromatin that is in a transcription-competent conformation. [PMID:32017156] |
receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
RNA polymerase II transcription regulator complex | cellular component | A transcription factor complex that acts at a regulatory region of a gene transcribed by RNA polymerase II. [GOC:tb] |
Involved In
This protein is involved in 46 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
nitrogen catabolite activation of transcription from RNA polymerase II promoter | biological process | A transcription regulation process in which the presence of one nitrogen source leads to an increase in the frequency, rate, or extent of transcription, from an RNA polymerase II promoter, of specific genes involved in the metabolism of other nitrogen sources. [GOC:mah, GOC:txnOH, PMID:19104072] |
intracellular glucose homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of glucose within a cell. [GOC:dph, GOC:go_curators, GOC:tb] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
cell-cell junction assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a junction between cells. [GOC:ai] |
Notch signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to the receptor Notch on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:go_curators, GOC:signaling] |
bile acid metabolic process | biological process | The chemical reactions and pathways involving bile acids, a group of steroid carboxylic acids occurring in bile, where they are present as the sodium salts of their amides with glycine or taurine. [GOC:go_curators] |
negative regulation of tumor necrosis factor-mediated signaling pathway | biological process | Any process that decreases the rate or extent of the tumor necrosis factor-mediated signaling pathway. The tumor necrosis factor-mediated signaling pathway is the series of molecular signals generated as a consequence of tumor necrosis factor binding to a cell surface receptor. [GOC:dph, GOC:tb] |
regulation of low-density lipoprotein particle clearance | biological process | Any process that modulates the rate, frequency or extent of low-density lipoprotein particle clearance. Low-density lipoprotein particle clearance is the process in which a low-density lipoprotein particle is removed from the blood via receptor-mediated endocytosis and its constituent parts degraded. [GOC:BHF, GOC:dph, GOC:tb] |
intracellular receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a receptor located within a cell. [GOC:bf, GOC:mah] |
negative regulation of type II interferon production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interferon-gamma production. Interferon-gamma is also known as type II interferon. [GOC:add, GOC:mah, PMID:15546383] |
negative regulation of interleukin-1 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-1 production. [GOC:mah] |
negative regulation of interleukin-2 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-2 production. [GOC:mah] |
negative regulation of interleukin-6 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-6 production. [GOC:mah] |
negative regulation of tumor necrosis factor production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of tumor necrosis factor production. [GOC:mah, PMID:10891884, PMID:15560120] |
positive regulation of interleukin-17 production | biological process | Any process that activates or increases the frequency, rate, or extent of production of any member of the interleukin-17 family of cytokines. [GOC:add, GOC:mah, PMID:16482511] |
toll-like receptor 9 signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to the endolysosomal toll-like receptor 9. [GOC:add, PMID:16551253, PMID:17328678] |
regulation of urea metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving urea. [GOC:mah] |
intracellular triglyceride homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of triglyceride within a cell. [GOC:BHF] |
positive regulation of insulin secretion involved in cellular response to glucose stimulus | biological process | Any process that increases the frequency, rate or extent of the regulated release of insulin that contributes to the response of a cell to glucose. [GOC:bf, GOC:yaf] |
bile acid signaling pathway | biological process | The series of molecular signals initiated by bile acid binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:signaling, PMID:12016314] |
intracellular bile acid receptor signaling pathway | biological process | The series of molecular signals initiated by a bile acid binding to an receptor located within a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, PMID:10334992] |
cholesterol homeostasis | biological process | Any process involved in the maintenance of an internal steady state of cholesterol within an organism or cell. [GOC:go_curators] |
defense response to bacterium | biological process | Reactions triggered in response to the presence of a bacterium that act to protect the cell or organism. [GOC:jl] |
negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
negative regulation of canonical NF-kappaB signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
positive regulation of insulin receptor signaling pathway | biological process | Any process that increases the frequency, rate or extent of insulin receptor signaling. [GOC:bf] |
fatty acid homeostasis | biological process | Any process involved in the maintenance of an internal steady state of fatty acid within an organism or cell. [GOC:BHF, GOC:rl] |
regulation of insulin secretion involved in cellular response to glucose stimulus | biological process | Any process that modulates the frequency, rate or extent of the regulated release of insulin that contributes to the response of a cell to glucose. [GOC:BHF, GOC:dph] |
regulation of bile acid biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of bile acids. [GOC:BHF, GOC:mah] |
cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
cellular response to fatty acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a fatty acid stimulus. [GOC:mah] |
cellular response to organonitrogen compound | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an organonitrogen stimulus. An organonitrogen compound is formally a compound containing at least one carbon-nitrogen bond. [GOC:mah] |
negative regulation of monocyte chemotactic protein-1 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of production of monocyte chemotactic protein-1. [GOC:mah] |
regulation of cholesterol metabolic process | biological process | Any process that modulates the rate, frequency, or extent of cholesterol metabolism, the chemical reactions and pathways involving cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:BHF, GOC:dph, GOC:tb] |
cellular response to bile acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a bile acid stimulus. [GO_REF:0000071, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:21757002] |
positive regulation of adipose tissue development | biological process | Any process that activates or increases the frequency, rate or extent of adipose tissue development. [GO_REF:0000058, GOC:TermGenie, PMID:23081848] |
positive regulation of phosphatidic acid biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidic acid biosynthetic process. [GO_REF:0000058, GOC:bc, GOC:PARL, GOC:TermGenie, PMID:23767959] |
positive regulation of glutamate metabolic process | biological process | Any process that activates or increases the frequency, rate or extent of glutamate metabolic process. [GOC:sl] |
positive regulation of ammonia assimilation cycle | biological process | Any process that activates or increases the frequency, rate or extent of ammonia assimilation cycle. [GOC:BHF] |
cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
negative regulation of inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai] |