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Activation of TGR5 (unknown origin) at 10 uM
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of mouse TGR5
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at GPBAR1 in human NCI-H716 cells
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Agonist activity at human TGR5
Agonist activity at mouse TGR5
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Agonist activity at human TGR5 relative to LCA
Agonist activity at TGR5 in rat Primary intestinal cell assessed as stimulation of GLP-1 secretion incubated for 2 hrs by ELISA analysis relative to control
Agonist activity at human TGR5 in human NCI-H716 cells assessed as stimulation of GLP-1 secretion incubated for 2 hrs by ELISA analysis relative to control
Agonist activity at human TGR5 expressed in human HEK293 cells at 20 uM measured after 5.5 hrs by steady-glo luciferase assay relative to control
Assay data:4 Tested
Agonist activity at human TGR5 expressed in human HEK293 cells measured after 5.5 hrs by steady-glo luciferase assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Agonist activity at TGR5 in human HEK293 cells assessed as increase in cAMP production
Assay data:14 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 14 Tested
Invivo agonist activity at TGR5 in mouse assessed as reduction in blood glucose level at 30 mg/kg, po relative to control
Invivo agonist activity at TGR5 in mouse assessed as reduction in insulin level at 30 mg/kg, po relative to control
Invivo agonist activity at TGR5 in mouse assessed as reduction in GLP-1 secretion level at 30 mg/kg, po relative to control
Agonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP production at 1 uM relative to control
Agonist activity at human TGR5 transfected in human NCI-H716 cells assessed as increase in cAMP production at 10 uM relative to control
Agonist activity at human TGR5 transfected in human NCI-H716 cells assessed as increase in GLP-1 secretion at 5 uM relative to control
Agonist activity at TGR5 in rat Primary intestinal cell assessed as stimulation of GLP-1 secretion at 30 uM relative to control
Agonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP production
Assay data:7 Active, 1 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
Agonist activity at TGR5 in human HEK293 cells incubated for 30 mins
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
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