Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assayAgonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at rat glucagon receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assayAgonist activity at rat glucagon receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assay
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysisDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
In vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagon
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Compound was tested for its ability to displace [125I]glucagon from the glucagon receptorCompound was tested for its ability to displace [125I]glucagon from the glucagon receptor
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Compound was evaluated for its ability to displace radiolabeled glucagon (inactive up to 100 uM)Compound was evaluated for its ability to displace radiolabeled glucagon (inactive up to 100 uM)
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMPAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMP
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Antagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulation
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAnt