| Assay ID | Title | Year | Journal | Article |
|---|
| AID1262447 | Selectivity index, ratio of IC50 for bovine serum FAP to IC50 for recombinant human DPP4 | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125866 | Unbound fraction in CD-1 mouse plasma at 1 to 100 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1323362 | Binding affinity to DPP4 (unknown origin) assessed as dissociation constant by SPR assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125876 | Inhibition of human ERG by MK-499 displacement binding analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1301059 | Total clearance in beagle dog at 1 mg/kg, iv or 2 mg/kg, po by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
| AID1125890 | Inhibition of QPP (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638375 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as increase in GLP1 levels at 1 mg/kg, po pretreated for 60 mins followed by glucose challenge and measured 5 to 10 mins post glucose challenge by OGTT relative to control | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1125870 | Ratio of drug level in brain to plasma in CD-1 mouse | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638343 | Binding affinity to DPP4 (unknown origin) expressed in baculovirus expressing system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1656016 | Cmax in ICR mouse at 2 mg/kg, po measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125881 | Toxicity in rat assessed as physical signs at 100 mg/kg/day, po for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262438 | Dose normalized AUC in rat at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1638366 | Anti-diabetic activity in ICR mouse assessed as inhibition of DPP4 in plasma at 3 mg/kg, po administered as single dose using Gly-Pro-AMC as substrate and measured after 7 days post dose by fluorometric assay relative to control | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1656020 | Ex-vivo inhibition of DPP4 in plasma isolated from ob/ob mouse treated at 30 mg/kg, po measured after 2 to 72 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125841 | Inhibition of DPP8 (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656013 | AUC (0 to t) in ICR mouse at 2 mg/kg, po measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1262433 | Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1262436 | Plasma clearance in rat at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125880 | Toxicity in rat assessed as mortality at 100 mg/kg/day, po for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656014 | Volume of distribution at steady state in ICR mouse at 0.5 mg/kg, iv measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1656015 | Half life in ICR mouse at 0.5 mg/kg, iv measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125872 | Ratio of drug level in brain to plasma in beagle dog | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656029 | Toxicity in ob/ob mouse assessed as induction of body weight gain at 30 mg/kg, po dosed once every three days for 31 days | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125871 | Ratio of drug level in brain to plasma in Sprague-Dawley rat | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125887 | Tmax in rat at 100 mg/kg/day, po administered for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262435 | Half life in rat at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125869 | Unbound fraction in human plasma at 1 to 100 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125840 | Inhibition of PEP (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262439 | Oral bioavailability in rat at 2 mg/kg | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1301062 | Oral bioavilability in beagle dog at 2 mg/kg | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
| AID1125868 | Unbound fraction in beagle dog plasma at 1 to 100 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638373 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po pretre at ed for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT rel at ive to con | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1638372 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 3 mg/kg, po pretre at ed for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT rel at ive to cont | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1301060 | Terminal half life in beagle dog at 1 mg/kg, iv or 2 mg/kg, po by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
| AID1125877 | Effect on potassium channel IKs (unknown origin) up to 30 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262434 | Inhibition of bovine serum FAP | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125884 | Toxicity in rat assessed as decrease in cholesterol level at 100 mg/kg/day, po for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656089 | Antidiabetic activity in ob/ob mouse assessed as reduction in decrease in HbA1c level at 30 mg/kg, po dosed once every three days for 31 day relative to control | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1323376 | In-vivo inhibition of DPP4 in ICR mouse at 5 mg/kg, ip administered as single dose using Gly-Pro-AMC as substrate after 24 hrs post dose by continuous fluorometric assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125889 | Competitive reversible inhibition of DPP4 (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125843 | Inhibition of potassium channel IKr (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262437 | Inhibition of potassium channel Cav1.2 (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1395907 | Elimination half life in human | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID1125891 | Inhibition of FAP (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638382 | Anti-diabetic activity in db/db mouse assessed as increase in glucose-induced insulin secretion at 10 mg/kg, po dosed once weekly for 8 weeks pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT r | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1125849 | In vivo inhibition of DPP4 in mouse plasma at 0.3 mg/kg, po | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638342 | Binding affinity to DPP4 (unknown origin) expressed in baculovirus expressing system assessed as dissociation rate constant | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1638379 | Anti-diabetic activity in db/db mouse assessed as reduction in fasting blood glucose at 10 mg/kg, po dosed once weekly for 8 weeks | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1125873 | Ratio of drug level in brain to plasma in human | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125886 | Cmax in rat at 100 mg/kg/day, po administered for for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638383 | Anti-diabetic activity in db/db mouse assessed as HbA1c levels at 10 mg/kg, po dosed once weekly for 8 weeks | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1638380 | Anti-diabetic activity in db/db mouse assessed as increase in glucose tolerance at 10 mg/kg, po dosed once weekly for 8 weeks by OGTT | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1656031 | Antidiabetic activity in ob/ob mouse assessed as reduction in decrease in HbA1c level at 3 to 30 mg/kg, po dosed once every three days for 31 day | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1638355 | Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS-MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1125883 | Toxicity in rat assessed as decrease in triglyceride level at 100 mg/kg/day, po for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1323384 | Improvement in glucose tolerance in ICR mouse assessed as reduction in glucose AUC (0 to 120 mins) at 10 mg/kg, po administered as single dose 60 mins before glucose challenge and measured 30 to 60 mins post glucose challenge by OGTT method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125842 | Inhibition of DPP9 (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125882 | Toxicity in rat assessed as decrease in glucose level at 100 mg/kg/day, po for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656027 | Antidiabetic activity in ob/ob mouse assessed as reduction in random blood glucose levels at 30 mg/kg, po dosed once every three days for 31 days | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1638377 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as increase in insulin levels at 1 mg/kg, po pretreated for 60 mins followed by glucose challenge by OGTT | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1656018 | Intrinsic clearance in mouse liver microsomes at 0.5 uM incubated for 0.5 to 60 mins by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125878 | Effect on sodium channel (unknown origin) up to 30 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1301063 | Dose normalized AUC in beagle dog at 2 mg/kg, po | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
| AID1323381 | In-vivo inhibition of DPP4 in B6.V-Lep'ob/Lep'ob (ob/ob) mouse at 3 mg/kg, po administered as single dose using Gly-Pro-AMC as substrate after 24 hrs post dose by continuous fluorometric assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125846 | Antidiabetic activity in po dosed lean mouse assessed as reduction in blood glucose excursion after 1 hr by oral glucose tolerance test | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125874 | Genotoxicity in Salmonella typhimurium by Ames mutagenicity test | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125845 | Inhibition of Nav1.5 (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262444 | Oral bioavailability in dog at 2 mg/kg | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1638340 | Binding affinity to DPP4 (unknown origin) expressed in baculovirus expressing system assessed as association rate constant | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1125851 | Inhibition of DPP4 in mouse plasma | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656021 | Ex-vivo inhibition of DPP4 in plasma isolated from ob/ob mouse assessed as time duration during which DPP4 inhibition rate stays above 80% treated at 30 mg/kg, po measured after 2 to 72 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1262432 | Inhibition of N-terminal FLAG tagged human QPP expressed in Sf9 cells using Nle-Pro-AMC substrate after 30 mins by plate reader analysis | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125848 | Antidiabetic activity in lean mouse assessed as reduction in blood glucose AUC at 0.3 mg/kg, po after 1 hr by oral glucose tolerance test | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125852 | Increase in active GLP1 (GLP-1(7-36)amide and GLP-1(7-37)) level in po dosed mouse plasma | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125867 | Unbound fraction in Sprague-Dawley rat plasma at 1 to 100 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1638370 | Anti-diabetic activity in 6 h-fasted db/db mouse assessed as inhibition of DPP4 in plasma at 10 mg/kg, po administered as single dose pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1323358 | Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125885 | AUC (0 to 24 hrs) in rat at 100 mg/kg/day, po administered for 14 days | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262442 | Half life in dog at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1262446 | Selectivity index, ratio of IC50 for C-terminal His-tagged DPP8 (unknown origin) to IC50 for recombinant human DPP4 | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125844 | Inhibition of Cav1.2 (unknown origin) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656012 | Half life in ICR mouse at 2 mg/kg, po measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1656011 | Clearance in ICR mouse at 0.5 mg/kg, iv measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1125879 | Effect on L-type Ca2+ channel (unknown origin) up to 30 uM | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1262440 | Inhibition of human ERG assessed as reduction in IKr current | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1323360 | Binding affinity to DPP4 (unknown origin) assessed as association rate constant by SPR assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1638371 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins)at 0.3 mg/kg, po pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT relative to control | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1262443 | Dose normalized AUC in dog at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1262445 | Selectivity index, ratio of IC50 for N-terminal FLAG tagged human QPP to IC50 for recombinant human DPP4 | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1262441 | Plasma clearance in dog at 1 mg/kg, iv and 2 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125875 | Inhibition of human ERG up to 30 uM by PatchXpress analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1656010 | Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1656017 | Oral bioavailability in ICR mouse at 2 mg/kg measured after 0.0833 to 120 hrs by LC-MS-MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1262431 | Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
| Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
| AID1125850 | Plasma concentration in mouse at 0.3 mg/kg, po | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1125847 | Antidiabetic activity in lean mouse assessed as reduction in blood glucose AUC at 0.01 mg/kg, po after 1 hr by oral glucose tolerance test | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| AID1323361 | Binding affinity to DPP4 (unknown origin) assessed as dissociation rate constant by SPR assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1345443 | Human dipeptidyl peptidase 4 (S9: Prolyl oligopeptidase) | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
| Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |