Assay ID | Title | Year | Journal | Article |
AID698522 | Tmax in C57bl/6 mouse at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595116 | Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay relative to 10 uM TUG-20 | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID698523 | Cmax in C57bl/6 mouse at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595115 | Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID673112 | Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
| Discovery of a potent and selective GPR120 agonist. |
AID1308063 | Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX- | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID595122 | Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID673111 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
| Discovery of a potent and selective GPR120 agonist. |
AID620370 | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. |
AID673123 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay relative to TUG-424 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
| Discovery of a potent and selective GPR120 agonist. |
AID698530 | Stability in human liver microsomes at 1 uM incubated for 60 mins by HPLC-MS/MS method | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595119 | Transactivation of human PPARgamma ligand binding domain transfected in mouse embryo fibroblasts assessed as renilla luciferase activity at 1 uM after 18 hrs by luminometry relative to 1 uM rosiglitazone | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID698539 | Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595117 | Transactivation of human PPARgamma ligand binding domain transfected in mouse embryo fibroblasts at 100 uM after 18 hrs analyzed by photinus and renilla luciferase activity by luminometry relative to 1 uM rosiglitazone | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID595170 | Agonist activity at human GPR41 in HEK293 cells | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID595121 | Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID698533 | Lipophilicity, log D of the compound at pH 7.4 by shake flask method | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID698535 | Agonist activity at GPR120 assessed as stimulation of calcium mobilization | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595123 | Induction of 12 mM glucose-stimulated insulin secretion in rat INS-1E cells at 10 uM after 1 hr by radioimmunoassay | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID698521 | AUC in C57bl/6 mouse at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID673122 | Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay relative to TUG-424 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
| Discovery of a potent and selective GPR120 agonist. |
AID595114 | Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition up to 1 hr by dynamic mass redistribution optical biosensor assay | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID1308064 | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID698532 | Agonist activity at GPR120 assessed as stimulation of calcium mobilization relative to TUG20 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595171 | Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID595169 | Agonist activity at human GPR43 in HEK293 cells | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID595165 | Induction of 2.8 mM glucose-stimulated insulin secretion in rat INS-1E cells at 10 uM after 1 hr by radioimmunoassay | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID1308065 | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay relative to TUG-770 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID698538 | Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization relative to TUG20 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. |
AID595166 | Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
AID595120 | Selectivity for human FFA1 over human PPARgamma | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7
| Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |