| Assay ID | Title | Year | Journal | Article |
|---|
| AID1346457 | Mouse GPBA receptor (Bile acid receptor) | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441581 | Cholerectic effect in bile fistula rat model assessed as maximum bile secretion rate at 1 umol/min/kg, iv over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441572 | Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID731376 | Agonist 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 immunoassay | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
| AID1059690 | Agonist activity at wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID774884 | Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay relative to control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold. |
| AID1059684 | Agonist activity at TGR5 N93A mutant (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID441575 | Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay relative to lithocholic acid | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID1741060 | Agonist 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 assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects. |
| AID1059689 | Selectivity ratio of EC50 for TGR5 E169A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID1698084 | Agonist activity at human TGR5 expressed in HEK293 cells measured after 30 mins by cAMP substrate based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis. |
| AID731382 | Metabolic stability in human liver microsomes assessed as intrinsic clearance measured per mg of protein | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
| AID1059692 | Selectivity ratio of EC50 for TGR5 N93A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID762282 | Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
| Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists. |
| AID441587 | Metabolic stability in human stool broth culture assessed as unmodified drug level after 12 hrs | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID1186284 | Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists. |
| AID1059683 | Agonist activity at TGR5 E169A mutant (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID1059679 | Agonist activity at TGR5 S270A mutant (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID441583 | Cholerectic effect in bile fistula rat model assessed as maximum bile secretion rate at 1 umol/min/kg administered intraduodenally over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441574 | Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay relative to INT-747 | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID673745 | Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis relative to 10 uM LCA | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID673746 | Agonist activity at GST-tagged FXR-LBD using biotinylated-SRC-1 peptide as substrate preincubated with compound for 30 mins measured after 4 hrs | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID441580 | Metabolic stability in bile fistula rat model assessed as conjugated drug level recovered in bile at 1 umol/min/kg administered intraduodenally over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID673751 | Binding affinity to albumin by equilibrium dialysis | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID1694293 | Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists. |
| AID441577 | Critical micellar concentration in 0.15 M NaCl water solution | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID673747 | Agonist 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 CDCA | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID441578 | Binding affinity to albumin | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID1686017 | Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay | 2016 | Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
| 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. |
| AID441590 | Induction of GLP1 release in high fat diet fed TGR5-Tg mouse Ileal mucosa explants | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441576 | Solubility in 0.1M HCl water solution | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID1694292 | Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists. |
| AID673750 | Aqueous solubility of the compound in 0.1 M HCl water at pH 3 by HPLC-ES-MS/MS | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID1741061 | Agonist 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 assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects. |
| AID441573 | Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441579 | Metabolic stability in bile fistula rat model assessed as intact drug level recovered in bile at 1 umol/min/kg administered intraduodenally over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441584 | Cholerectic 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 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID441582 | Cholerectic 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 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID731387 | Agonist 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 immunoassay | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
| AID673744 | Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID1059688 | Selectivity ratio of EC50 for TGR5 Y89A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID441585 | Metabolic stability in bile fistula rat model assessed as intact drug level recovered in bile at 1 umol/min/kg, iv over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID731373 | Lipophilicity, log D of the compound by by shake-flask method | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
| AID441586 | Metabolic stability in bile fistula rat model assessed as conjugated drug level recovered in bile at 1 umol/min/kg, iv over 1 hr | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| 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. |
| AID774885 | Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold. |
| AID1059687 | Selectivity ratio of EC50 for TGR5 N76A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID731375 | Agonist 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 immunoassay | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
| AID710115 | Gall bladder toxicity in normal mouse assessed as increase in gall bladder volume at 60 mg/kg relative to untreated control | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. |
| AID1059678 | Agonist activity at TGR5 N76A mutant (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID673748 | Critical micelle concentration of the compound in 0.15 M NaCl water solution | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| AID774890 | Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold. |
| AID1686015 | Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay | 2016 | Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
| 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. |
| AID1386215 | Toxicity 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 mins | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5). |
| AID1059685 | Selectivity ratio of EC50 for TGR5 S270A mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID1059686 | Selectivity ratio of EC50 for TGR5 Y89F mutant (unknown origin) to EC50 for wild type TGR5 (unknown origin) | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Probing the Binding Site of Bile Acids in TGR5. |
| AID774888 | Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay relative to control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold. |
| AID1686018 | Agonist 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 LCA | 2016 | Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
| 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. |
| AID673749 | 1-Octanol/water partition coefficient, log P of the compound by conventional shake-flask method | 2012 | ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
| Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |