Compounds > int-777
Page last updated: 2024-08-03 16:17:14

int-777

Description

Cross-References

ID SourceID
PubMed CID45483949
CHEMBL ID567640
SCHEMBL ID593390
MeSH IDM0541646

Synonyms (27)

Synonym
CHEMBL567640 ,
6alpha-ethyl-23(s)-methyl-cholic acid
bdbm50300199
1199796-29-6
int 777
s-emca
cholane-23-carboxylic acid, 6-ethyl-3,7,12-trihydroxy-, (3alpha,5beta,6alpha,7alpha,12alpha,23s)-
int-777
utd8bcw6b8 ,
unii-utd8bcw6b8
6alpha-ethyl-23(s)-methylcholic acid
int777
gtpl7048
(2s,4r)-4-[(3r,5s,6r,7r,8r,9s,10s,12s,13r,14s,17r)-6-ethyl-3,7,12-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid
SCHEMBL593390
HY-15677
CS-3199
6.alpha.-ethyl-23(s)-methylcholic acid
6a-ethyl-23(s)-methylcholic acid
AC-31549
AKOS027384000
6alpha-ethyl-23(s)-methyl-3alpha,7alpha,12alpha-trihydroxy-5beta-cholan-24-oic acid
Q27088779
(2s,4r)-4-[(3r,5s,6r,7r,8r,9s,10s,12s,13r,14s,17r)-6-ethyl-10,13-dimethyl-3,7,12-tris(oxidanyl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methyl-pentanoic acid
FX0 ,
MS-28184
ZXB79629

Protein Targets (4)

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Cytochrome P450 2C9 Homo sapiens (human)EC500.2930AID1186284
G-protein coupled bile acid receptor 1Mus musculus (house mouse)EC500.2477AID1694293; AID1741061; AID774885
G-protein coupled bile acid receptor 1Homo sapiens (human)EC502.2907AID1059690; AID1186284; AID1686017; AID1694292; AID1698084; AID1741060; AID441573; AID673744; AID731376; AID731387; AID762282; AID774890
Bile acid receptorHomo sapiens (human)EC50100.0000AID1686015; AID441572; AID673746

Bioassays (58)

Assay IDTitleYearJournalArticle
AID1346457Mouse GPBA receptor (Bile acid receptor)2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441581Cholerectic effect in bile fistula rat model assessed as maximum bile secretion rate at 1 umol/min/kg, iv over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441572Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID731376Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
ISSN: 1948-5875		Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
AID1059690Agonist activity at wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID774884Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay relative to control2013European journal of medicinal chemistry, Nov, Volume: 69ISSN: 1768-3254Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
AID1059684Agonist activity at TGR5 N93A mutant (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID441575Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay relative to lithocholic acid2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID1741060Agonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay2020European journal of medicinal chemistry, Oct-01, Volume: 203ISSN: 1768-3254Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
AID1059689Selectivity ratio of EC50 for TGR5 E169A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID1698084Agonist activity at human TGR5 expressed in HEK293 cells measured after 30 mins by cAMP substrate based assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
ISSN: 1520-4804		Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
AID731382Metabolic stability in human liver microsomes assessed as intrinsic clearance measured per mg of protein2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
ISSN: 1948-5875		Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
AID1059692Selectivity ratio of EC50 for TGR5 N93A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID762282Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
ISSN: 1464-3405		Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists.
AID441587Metabolic stability in human stool broth culture assessed as unmodified drug level after 12 hrs2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID1186284Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
ISSN: 1464-3405		Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.
AID1059683Agonist activity at TGR5 E169A mutant (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID1059679Agonist activity at TGR5 S270A mutant (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID441583Cholerectic effect in bile fistula rat model assessed as maximum bile secretion rate at 1 umol/min/kg administered intraduodenally over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441574Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay relative to INT-7472009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID673745Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis relative to 10 uM LCA2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID673746Agonist activity at GST-tagged FXR-LBD using biotinylated-SRC-1 peptide as substrate preincubated with compound for 30 mins measured after 4 hrs2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID441580Metabolic stability in bile fistula rat model assessed as conjugated drug level recovered in bile at 1 umol/min/kg administered intraduodenally over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID673751Binding affinity to albumin by equilibrium dialysis2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID1694293Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32ISSN: 1464-3391Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.
AID441577Critical micellar concentration in 0.15 M NaCl water solution2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID673747Agonist activity at GST-tagged FXR-LBD using biotinylated-SRC-1 peptide as substrate preincubated with compound for 30 mins measured after 4 hrs relative to 10 uM CDCA2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID441578Binding affinity to albumin2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID1686017Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay2016Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
ISSN: 1520-4804		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.
AID441590Induction of GLP1 release in high fat diet fed TGR5-Tg mouse Ileal mucosa explants2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441576Solubility in 0.1M HCl water solution2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID1694292Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32ISSN: 1464-3391Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.
AID673750Aqueous solubility of the compound in 0.1 M HCl water at pH 3 by HPLC-ES-MS/MS2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID1741061Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay2020European journal of medicinal chemistry, Oct-01, Volume: 203ISSN: 1768-3254Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
AID441573Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441579Metabolic stability in bile fistula rat model assessed as intact drug level recovered in bile at 1 umol/min/kg administered intraduodenally over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441584Cholerectic effect in bile fistula rat model assessed as maximum bile acids secretion rate per kg body weight at 1 umol/min/kg administered intraduodenally over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID441582Cholerectic effect in bile fistula rat model assessed as maximum bile acids secretion rate per kg body weight at 1 umol/min/kg, iv over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID731387Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
ISSN: 1948-5875		Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
AID673744Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID1059688Selectivity ratio of EC50 for TGR5 Y89A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID441585Metabolic stability in bile fistula rat model assessed as intact drug level recovered in bile at 1 umol/min/kg, iv over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID731373Lipophilicity, log D of the compound by by shake-flask method2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
ISSN: 1948-5875		Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
AID441586Metabolic stability in bile fistula rat model assessed as conjugated drug level recovered in bile at 1 umol/min/kg, iv over 1 hr2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
ISSN: 1520-4804		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.
AID774885Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay2013European journal of medicinal chemistry, Nov, Volume: 69ISSN: 1768-3254Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
AID1059687Selectivity ratio of EC50 for TGR5 N76A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID731375Agonist activity at dog TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay2013ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
ISSN: 1948-5875		Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
AID710115Gall bladder toxicity in normal mouse assessed as increase in gall bladder volume at 60 mg/kg relative to untreated control2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
ISSN: 1520-4804		Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists.
AID1059678Agonist activity at TGR5 N76A mutant (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID673748Critical micelle concentration of the compound in 0.15 M NaCl water solution2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
AID774890Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay2013European journal of medicinal chemistry, Nov, Volume: 69ISSN: 1768-3254Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
AID1686015Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay2016Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
ISSN: 1520-4804		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.
AID1386215Toxicity in overnight fasted CD1 mouse assessed as inhibition of egg yolk-stimulated gall bladder emptying at 30 mg/kg, po pre-treated 1 hr 45 mins before egg yolk feeding and measured after 15 mins2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
ISSN: 1520-4804		Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5).
AID1059685Selectivity ratio of EC50 for TGR5 S270A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID1059686Selectivity ratio of EC50 for TGR5 Y89F mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin)2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
ISSN: 1948-5875		Probing the Binding Site of Bile Acids in TGR5.
AID774888Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay relative to control2013European journal of medicinal chemistry, Nov, Volume: 69ISSN: 1768-3254Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
AID1686018Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay relative to 10 uM LCA2016Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
ISSN: 1520-4804		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.
AID6737491-Octanol/water partition coefficient, log P of the compound by conventional shake-flask method2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
ISSN: 1948-5875		Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.

Research

Studies (47)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (4.26)29.6817
2010's30 (63.83)24.3611
2020's15 (31.91)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (4.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other45 (95.74%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
furafylline
1
oxopurine2014201410.0low000010
ketoconazole
1
dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine		2014201410.0low000010
sulfaphenazole
1
primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor		2014201410.0low000010
lithocholic acid
3
bile acid;
C24-steroid;
monohydroxy-5beta-cholanic acid		geroprotector;
human metabolite;
mouse metabolite		2012201610.3low000030
chenodeoxycholic acid
4
bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		2009201611.5low000130
ursodeoxycholic acid
1
bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		201620168.0low000010
cholic acid
4
12alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		2009201611.5low000130
quinidine
1
cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker		2014201410.0low000010
tretinoin
1
retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule		201620168.0low000010
sr 12813
1
organic phosphonate;
phenols		pregnane X receptor agonist201620168.0low000010
obeticholic acid
4
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
dihydroxy-5beta-cholanic acid		farnesoid X receptor agonist;
hepatoprotective agent		200920209.5low000130
t0901317
2
201620206.0low000020
alitretinoin
2
retinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist		201620206.0low000020
tamoxifen
1
stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator		201620168.0low000010
gw 7647
1
aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist201620168.0low000010
calcitriol
1
D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical		201620168.0low000010
pulmicort
1
11beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen		201620168.0low000010
gw 1929
1
benzophenones201620168.0low000010
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde o-(3,4-dichlorobenzyl)oxime
1
201620168.0low000010
gw 4064
1
stilbenoid202020204.0low000010
gw0742
1
monocarboxylic acid201620168.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
adenine
1
6-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite		202120213.0low000001
nitrates
1
monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species		202020204.0low000010
1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine
1
methylpyridines;
phenylpyridine;
tetrahydropyridine		neurotoxin202220222.0low000001
fenofibrate
1
aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic		201820186.0low000010
taurocholic acid
2
amino sulfonic acid;
bile acid taurine conjugate		human metabolite201120199.0low000020
lithocholic acid
2
bile acid;
C24-steroid;
monohydroxy-5beta-cholanic acid		geroprotector;
human metabolite;
mouse metabolite		201120189.5low000020
chenodeoxycholic acid
6
bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		201820215.2low000051
oleanolic acid
1
hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite2012201212.0low000010
phenyl acetate
1
benzenes;
phenyl acetates		201820186.0low000010
ursodeoxycholic acid
1
bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		202020204.0low000010
bezafibrate
1
aromatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic		201820186.0low000010
1-methyl-4-phenylpyridinium
1
pyridinium ionapoptosis inducer;
herbicide;
human xenobiotic metabolite;
neurotoxin		202220222.0low000001
mci-196
1
2012201212.0low000010
triazoles
1
1,2,3-triazole201820186.0low000010
u 73122
2
aromatic ether;
aza-steroid;
maleimides		EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor2012201610.0low000020
24-norursodeoxycholic acid
1
202020204.0low000010
deoxycholic acid
1
bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human blood serum metabolite201920195.0low000010
esi-05
1
201620168.0low000010
obeticholic acid
6
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
dihydroxy-5beta-cholanic acid		farnesoid X receptor agonist;
hepatoprotective agent		201820215.2low000051
h 89
1
N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide202320231.0low000001
sphingosine
1
sphing-4-eninehuman metabolite;
mouse metabolite		201620168.0low000010
sphingosine 1-phosphate
1
sphingoid 1-phosphatemouse metabolite;
signalling molecule;
sphingosine-1-phosphate receptor agonist;
T-cell proliferation inhibitor;
vasodilator agent		201620168.0low000010
ceruletide
1
oligopeptidediagnostic agent;
gastrointestinal drug		201820186.0low000010
glucagon-like peptide 1
3
2009201611.7low000120
9-(tetrahydro-2-furyl)-adenine
1
202120213.0low000001
ncx1000
1
202020204.0low000010
tauromuricholate
1
2011201113.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acquired Nephrogenic Diabetes Insipidus0
1
201820186.0low000010
Acute Brain Injuries0
1
201920195.0low000010
Acute Edematous Pancreatitis0
1
201820186.0low000010
Acute Liver Injury, Drug-Induced0
1
202020204.0low000010
Age-Related Osteoporosis0
1
202120213.0low000001
Albuminuria0
1
201820186.0low000010
Alloxan Diabetes0
2
201620187.0low000020
Alopecia Areata0
1
202120213.0low000001
Alopecia Circumscripta0
1
202120213.0low000001
Anxiety0
1
202120213.0low000001
Atherogenesis0
1
2011201113.0low000010
Atherosclerosis0
1
2011201113.0low000010
Atherosclerotic Parkinsonism0
1
202220222.0low000001
Bile Duct Cancer0
1
201820186.0low000010
Bile Duct Neoplasms0
1
201820186.0low000010
Biliary Cirrhosis0
2
201820205.0low000020
Biliary Tract Diseases0
1
2011201113.0low000010
Blood Poisoning0
1
202120213.0low000001
Brain Inflammation0
2
201920214.0low000011
Brain Injuries0
1
201920195.0low000010
Cancer of Lung0
1
202220222.0low000001
Carcinoma, Non-Small Cell Lung0
1
202220222.0low000001
Carcinoma, Non-Small-Cell Lung0
1
202220222.0low000001
Cardiac Failure0
1
201820186.0low000010
Cerebral Infarction, Middle Cerebral Artery0
1
202120213.0low000001
Chemical and Drug Induced Liver Injury0
1
202020204.0low000010
Cholangiocarcinoma0
1
201820186.0low000010
Cholangiocellular Carcinoma0
1
201820186.0low000010
Chronic Hepatitis B0
1
202120213.0low000001
Cirrhosis0
2
201620187.0low000020
Cognition Disorders0
1
201920195.0low000010
Cognitive Decline0
1
202120213.0low000001
Cognitive Dysfunction0
1
202120213.0low000001
Colitis0
1
202020204.0low000010
Diabetes Mellitus0
1
2009200915.0low000100
Diabetes Mellitus, Adult-Onset0
2
201620187.0low000020
Diabetes Mellitus, Type 20
2
201620187.0low000020
Diabetic Glomerulosclerosis0
3
201620187.3low000030
Diabetic Nephropathies0
3
201620187.3low000030
Disease Exacerbation0
2
201820186.0low000020
Disease Models, Animal0
10
201120225.3low000064
Encephalitis0
2
201920214.0low000011
Endometrioma0
1
201920195.0low000010
Endometriosis0
1
201920195.0low000010
Fatty Liver, Nonalcoholic0
1
202020204.0low000010
Fibrosis0
2
201620187.0low000020
Heart Failure0
1
201820186.0low000010
Hemorrhage, Subarachnoid0
2
201920214.0low000011
Hepatitis B, Chronic0
1
202120213.0low000001
Infarction, Middle Cerebral Artery0
1
202120213.0low000001
Inflammation0
1
201920195.0low000010
Injury, Ischemia-Reperfusion0
1
202120213.0low000001
Innate Inflammatory Response0
1
201920195.0low000010
Insulin Resistance0
3
201220198.3low000030
Insulin Sensitivity0
3
201220198.3low000030
Itching0
1
201820186.0low000010
Kidney Diseases0
1
201620168.0low000010
Liver Cirrhosis, Biliary0
2
201820205.0low000020
Liver Diseases0
2
201120218.0low000011
Liver Dysfunction0
2
201120218.0low000011
Lung Neoplasms0
1
202220222.0low000001
Muscle Relaxation0
1
2011201113.0low000010
Necrosis0
1
201820186.0low000010
Non-alcoholic Fatty Liver Disease0
1
202020204.0low000010
Obesity0
5
200920199.2low000140
Osteoarthritis of Knee0
1
201820186.0low000010
Osteoarthritis, Knee0
1
201820186.0low000010
Osteoporosis0
1
202120213.0low000001
Pancreatitis0
1
201820186.0low000010
Parkinson Disease, Secondary0
1
202220222.0low000001
Peripheral Nerve Injuries0
1
202320231.0low000001
Peripheral Nerve Injury0
1
202320231.0low000001
Pruritus0
1
201820186.0low000010
Reperfusion Injury0
1
202120213.0low000001
Sepsis0
1
202120213.0low000001
Subarachnoid Hemorrhage0
2
201920214.0low000011

Long-term Use (1)

ArticleYear
Differential effects of FXR or TGR5 activation in cholangiocarcinoma progression.
Biochimica et biophysica acta. Molecular basis of disease, , Volume: 1864, Issue:4 Pt B		2018

Bioavailability (1)

ArticleYear
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1		2013