| Assay ID | Title | Year | Journal | Article |
|---|
| AID693749 | Inhibition of human CYP2E1 in liver microsomes assessed as chlorzoxazone 6beta-hydroxylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID638011 | Cytotoxicity against human THLE cells after 72 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity. |
| AID693971 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as suppression of blood glucose level at 3 mg/kg/day measured on day 3 relative to control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693752 | Plasma clearance in mouse at 1 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693768 | Volume of distribution at steady state in monkey at 0.5 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693994 | Toxicity in rat at <= 100 mg/kg/day for 5 weeks by antemortem analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246552 | Antidiabetic activity in type-2 diabetic human model assessed as reduction in HbA1c level at 40 mg, qd administered for 12 weeks measured after post last dose relative to control | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693804 | Antidiabetic activity in mouse expressing human GCGR assessed as suppression of blood glucose AUC (0 to 24 mins) at 30 mg/kg, po administered 1 hour prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693964 | Plasma concentration in rhesus monkey at 0.3 mg/kg administered via nasogastric tube measured at 4 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693766 | Dose normalized AUC in dog at 0.5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693762 | Plasma clearance in dog at 0.5 mg/kg, iv and 0.5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID637992 | Displacement of [125I]Glucagon-Cex from human GCGR | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity. |
| AID693757 | Plasma clearance in rat at 2 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246553 | Antidiabetic activity in type-2 diabetic human model assessed as reduction in HbA1c level at 60 mg, qd administered for 12 weeks measured after post last dose relative to control | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693802 | Antidiabetic activity in mouse expressing human GCGR assessed as suppression of blood glucose AUC (0 to 24 mins) at 3 mg/kg, po administered 1 hour prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693739 | Antagonist activity at human VPAC2 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 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693763 | Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 0.5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246555 | Half life in human | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID1246551 | Antidiabetic activity in type-2 diabetic human model assessed as reduction in HbA1c level at 20 mg, qd administered for 12 weeks measured after post last dose relative to control | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693761 | Dose normalized AUC in rat at 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693977 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as suppression of blood glucose level at 10 mg/kg/day measured on day 10 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246554 | Antidiabetic activity in type-2 diabetic human model assessed as reduction in HbA1c level at 80 mg, qd administered for 12 weeks measured after post last dose relative to control | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693765 | Oral bioavailability in dog at 0.5 mg/kg | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693969 | Antidiabetic activity in ob/ob mouse expressing human GCGR assessed as suppression of blood glucose level at 1 mg/kg, po measured at 6 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693974 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as suppression of blood glucose level at 10 mg/kg/day measured on day 3 relative to control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693748 | Inhibition of human CYP2B6 in liver microsomes assessed as bupropion hydroxylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693973 | Cardiovascular toxicity in anesthetized dog up to 10 mg/kg, iv | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696515 | 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 counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID746494 | Cytotoxicity against human THLE cells assessed as ATP depletion after 72 hrs | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus. |
| AID693771 | Dose normalized AUC in monkey at 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693806 | Drug uptake in mouse expressing human GCGR at 3 mg/kg, po measured at 60 mins | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696513 | Antagonist activity at rhesus monkey 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 count | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693966 | Plasma concentration in rhesus monkey at 3 mg/kg administered via nasogastric tube measured at 4 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693961 | Antidiabetic activity in rhesus monkey assessed as reduction of glucagon-induced glucose label at 0.3 mg/kg administered 4 hrs via nasogastric tube prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693751 | Competitive inhibition of human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge by Schild plot method | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693993 | Cmax in rat at <= 100 mg/kg/day | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693740 | Binding affinity to human ERG | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693976 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as suppression of blood glucose level at 3 mg/kg/day measured on day 10 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693760 | Oral bioavailability in rat at 2 mg/kg | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693756 | Dose normalized AUC in mouse at 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693985 | Effect on CNS in conscious mouse at 100 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693801 | Plasma protein binding in human | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693980 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as blood glucagon level at 3 mg/kg/day measured on day 11 (Rvb = 445 +/- 55 pg/ml) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1128254 | Antidiabetic activity in human assessed as inhibition of exogenous glucagon-stimulated glucose excursion at 1000 mg, po qd relative to control | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist. |
| AID693990 | Reduction of HbA1c level in type2 diabetic patients at 80 mg, qd relative to baseline | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693986 | Inhibition of glucagon-induced glucose excursion in diabetic patients at 200 mg, qd | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696508 | Antagonist activity at human PAC1 expressed in mouse HIN 3T3 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 cou | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693809 | Antagonist activity at human GCGR expressed in mouse perfused liver model assessed as inhibition of glucagon-induced glycogenolysis at 0.1 uM administered 20 mins prior to glucagon challenge | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693798 | Plasma protein binding in rat | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693968 | Antidiabetic activity in ob/ob mouse expressing human GCGR assessed as suppression of blood glucose level at 1 mg/kg, po measured at 1 and 2 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693995 | Toxicity in rat at <= 100 mg/kg/day for 5 weeks by postmortem analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693978 | Plasma concentration in DIO mouse expressing human GCGR at 3 mg/kg/day measured on day 5 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID637993 | Antagonist activity at human GCGR assessed as inhibition of glucagon-induced cAMP accumulation in cell-based assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity. |
| AID696509 | Antagonist activity at human GLP1R 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 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696516 | Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693987 | Inhibition of glucagon-induced glucose excursion in diabetic patients at 1000 mg, qd | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693958 | Antagonist activity at human GCGR expressed in mouse perfused liver model assessed as inhibition of glucagon-induced glycogenolysis at 0.3 uM administered 20 mins prior to glucagon challenge | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693767 | Plasma clearance in monkey at 0.5 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693758 | Volume of distribution at steady state in rat at 2 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1128253 | Antidiabetic activity in human assessed as inhibition of exogenous glucagon-stimulated glucose excursion at 200 mg, po qd relative to control | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist. |
| AID693742 | Inhibition of Nav1.5 at 10 uM | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693965 | Plasma concentration in rhesus monkey at 1 mg/kg administered via nasogastric tube measured at 4 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693750 | Reversible inhibition of human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge by Schild plot method | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696510 | Antagonist activity at rat 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 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693800 | Plasma protein binding in monkey | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693983 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as total blood GLP1 level at 10 mg/kg/day measured on day 11 (Rvb = 46 +/- 4 pM) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693808 | Drug uptake in mouse expressing human GCGR at 30 mg/kg, po measured at 60 mins | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID746519 | Antagonist activity at human glucagon receptor assessed as inhibition of glucagon-induced cAMP production by cell based assay in presence of 4% bovine serum albumin | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus. |
| AID696514 | Antagonist activity at human GIPR 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 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246565 | Hypoglycemic activity in human assessed as time required to glucose recovery from 50 mg/dl to >= 70 mg/dl at 1 g (Rvb = 33.3 min) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693753 | Volume of distribution at steady state in mouse at 1 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693975 | Antidiabetic activity in GCGR knockout mouse assessed as increase in blood glucagon level relative to DIO mouse expressing human GCGR | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693803 | Antidiabetic activity in mouse expressing human GCGR assessed as suppression of blood glucose AUC (0 to 24 mins) at 10 mg/kg, po administered 1 hour prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693807 | Drug uptake in mouse expressing human GCGR at 10 mg/kg, po measured at 60 mins | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693770 | Oral bioavailability in monkey at 2 mg/kg | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693745 | Inhibition of human CYP2C8 in liver microsomes assessed as paclitaxel 6alpha-hydroxylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693982 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as total blood GLP1 level at 3 mg/kg/day measured on day 11 (Rvb = 46 +/- 4 pM) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693963 | Antidiabetic activity in rhesus monkey assessed as reduction of glucagon-induced glucose label at 3 mg/kg administered 4 hrs via nasogastric tube prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693799 | Plasma protein binding in dog | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693979 | Plasma concentration in DIO mouse expressing human GCGR at 10 mg/kg/day measured on day 5 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693755 | Oral bioavailability in mouse at 2 mg/kg | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696518 | Antagonist activity at human VPAC1 expressed in HT-29 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 | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696512 | 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 counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693764 | Elimination half life in dog at 0.5 mg/kg, iv and 0.5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693759 | Elimination half life in rat at 2 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693988 | Reduction of plasma glucose level in type2 diabetic patients at 60 mg, qd relative to baseline | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693741 | Displacement of [3H]diltiazem from L-type Ca2+ channel | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693959 | Antagonist activity at human GCGR expressed in mouse perfused liver model assessed as inhibition of glucagon-induced glycogenolysis at 1 uM administered 20 mins prior to glucagon challenge | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693744 | Inhibition of human CYP2D6 in liver microsomes assessed as dextromethorphan O-demethylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693972 | Toxicity in DIO mouse expressing human GCGR assessed as morphological changes in pancreatic tissues | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693746 | Inhibition of human CYP2C9 in liver microsomes assessed as diclofenac 4'-hydroxylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693989 | Reduction of plasma glucose level in type2 diabetic patients at 80 mg, qd relative to baseline | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693967 | Antidiabetic activity in ob/ob mouse expressing human GCGR assessed as suppression of blood glucose AUC (0 to 6 hrs) at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1390457 | Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities. |
| AID696517 | Reduction of HbA1c level in type2 diabetic patients at 60 mg, qd relative to baseline | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1390458 | Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities. |
| AID693962 | Antidiabetic activity in rhesus monkey assessed as reduction of glucagon-induced glucose label at 1 mg/kg administered 4 hrs via nasogastric tube prior to glucagon challenge relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693769 | Elimination half life in monkey at 0.5 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693754 | Elimination half life in mouse at 1 mg/kg, iv and 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693981 | Antidiabetic activity in DIO mouse expressing human GCGR assessed as blood glucagon level at 10 mg/kg/day measured on day 11 (Rvb = 445 +/- 55 pg/ml) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693984 | Drug uptake in anesthetized dog up to 10 mg/kg, iv | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246566 | Hypoglycemic activity in type-2 diabetic human assessed as time required to glucose recovery from 50 mg/dl to >= 63 mg/dl at 1 g in presence of beta blocker propranolol (Rvb = 71 min) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693747 | Inhibition of human CYP1A2 in liver microsomes assessed as phenacetin O-deethylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693970 | Antidiabetic activity in ob/ob mouse expressing human GCGR assessed as suppression of blood glucose level at 0.3 mg/kg, po measured at 1, 3 and 6 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1246564 | Hypoglycemic activity in human assessed as time required to glucose recovery from 50 mg/dl to >= 70 mg/dl at 200 mg (Rvb = 33.3 min) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress in the development of small-molecule glucagon receptor antagonists. |
| AID693960 | Antagonist activity at human GCGR expressed in mouse perfused liver model assessed as inhibition of glucagon-induced glycogenolysis at 3 uM administered 20 mins prior to glucagon challenge | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID696511 | 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 counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693743 | Inhibition of human CYP3A4 in liver microsomes assessed as testosterone 6beta-hydroxylation after 48 hrs | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID693805 | Antidiabetic activity in ob/ob mouse expressing human GCGR assessed as suppression of blood glucose AUC (0 to 6 hrs) at 3 mg/kg, po | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1345960 | Human GIP receptor (Glucagon receptor family) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1346459 | Human PAC1 receptor (VIP and PACAP receptors) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1345985 | Human glucagon receptor (Glucagon receptor family) | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. |
| AID1805801 | Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\ | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Perspectives on SARS-CoV-2 Main Protease Inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |