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Binding affinity towards human GCGR in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:297 Tested
SummaryRelated BioAssays by Target
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation relative to glucagon
Assay data:10 Tested
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
Assay data:11 Active, 5 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
Inhibition of human GCGR receptor
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysis
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay relative to control
Assay data:18 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
Assay data:17 Active, 11 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
Assay data:6 Active, 6 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
Assay data:13 Active, 13 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
Antagonist activity at GCCR (unknown origin) expressed in HEK293 cells assessed as inhibition of GCG binding by measuring increase in fluorescence intensity at 0.1 mM incubated for 30 to 40 mins by FLUO-4 AM based inverted fluorescence microscopic imaging analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as inhibition of GCG binding by measuring increase in fluorescence intensity at 10 uM incubated for 30 to 40 mins by FLUO-4 AM fluorescence based flow cytometric analysis
Binding Assay from US Patent US9359339: "Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use"
Assay data:19 Active, 6 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding Assay from US Patent US8748624: "Picolinamido-propanoic acid derivatives useful as glucagon receptor antagonists"
Assay data:136 Active, 135 Activity ≤ 1 µM, 138 Tested
Binding Assay from US Patent US8691856: "Glucagon receptor antagonists, preparation and therapeutic uses"
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Glucagon Receptor Binding Assay from US Patent US8633231: "Substituted imidazolones, compositions containing such compounds and methods of use"
Assay data:20 Active, 3 Activity ≤ 1 µM, 20 Tested
SPA Receptor Binding Assay from Article 10.1021/jm8016249: "Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties."
Assay data:30 Active, 30 Activity ≤ 1 µM, 30 Tested
PRESTO-Tango GPCRome screening (GCGR)
Assay data:1 Tested
GLUCAGONH_AGON Cerep selectivity data (BI)
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production relative to control
Assay data:2 Tested
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