Assay ID | Title | Year | Journal | Article |
AID697663 | fCmax in dog at 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697648 | Fraction unbound in rat pancreas at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697868 | Activation of human hexokinase 1 at 500 times EC50 concentration | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697875 | Antidiabetic activity in Goto-Kakizaki rat assessed as decrease in fasting plasma glucose level at 100 mg/kg, po administered once daily measured on day 28 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697676 | Drug excretion in rat bile | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697863 | Drug uptake by rat hepatic OATP1A4 transporters expressed in CHO cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697660 | fAUC (0 to 24 hrs) in dog at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697677 | Renal excretion in rat | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697678 | Fraction absorbed in portal vein cannulated rat at 5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697649 | Fraction unbound in dog pancreas at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697670 | fCmax in monkey at 0.5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697882 | Antidiabetic activity in Goto-Kakizaki rat assessed as change in glycogen level at 10 to 100 mg/kg, po QD administered 60 mins before glucose challenge for 28 days by OGTT | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698001 | Lipophilicity, log D of the compound at pH 7.4 by by shake flask method | | | |
AID1059152 | Apparent permeability in RRCK cells at pH 5.5 | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697647 | Fraction unbound in dog liver at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1059149 | Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as active uptake | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697669 | fAUC (0 to 24 hrs) in monkey at 3 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697686 | Ratio of free drug uptake in liver to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697879 | Antidiabetic activity in Goto-Kakizaki rat assessed as decrease in glucose AUC at 100 mg/kg, po QD administered 60 mins before glucose challenge for 28 days by OGTT | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697679 | Thermodynamic solubility of the compound at pH 6.5 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697681 | Passive permeability across dog RRCK cells at pH 7.4 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697878 | Antidiabetic activity in po dosed Goto-Kakizaki rat assessed as decrease in postprandial plasma glucose level dosed once daily for 28 days administered 60 mins before glucose challenge for 28 days by OGTT | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697685 | Ratio of free drug uptake in liver to pancreas of Wistar rat at 100 mg/kg, po administered for 28 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698002 | Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis | | | |
AID1059153 | Apparent permeability in RRCK cells at pH 6.5 | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID1059150 | Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as passive uptake | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697661 | fAUC (0 to 24 hrs) in dog at 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697688 | Ratio of free drug uptake in brain to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697869 | Activation of human hexokinase 2 at 500 times EC50 concentration | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697867 | Drug uptake by human hepatic OATP2B1 transporters expressed in HEK cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697871 | Induction of glucokinase translocation from nucleus to cytoplasm in cryopreserved rat hepatocytes after 1 hr by Hoechst staining-based fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697642 | Fraction unbound in rat plasma at 50 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698015 | Hepatic clearance in human administered through oral dosing | | | |
AID1698000 | Apparent permeability in dog MDCKII-LE cells at pH 7.4 | | | |
AID1059183 | Lipophilicity, log D of the compound at pH 7.4 | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697651 | Fraction unbound in dog brain at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697687 | Ratio of free drug uptake in pancreas to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697650 | Fraction unbound in rat brain at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697644 | Fraction unbound in monkey plasma at 50 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697873 | Activation of glucokinase in Sprague-Dawley rat islets assessed as enhancement of glucose-stimulated insulin secretion at 100 times EC50 concentration after 60 mins by enzyme immunoassay | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697652 | fAUC (0 to 24 hrs) in rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697638 | Ratio of EC50 for activation of glucokinase in rat INS-1 cells to EC50 for in-vitro activation of rat glucokinase | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697671 | fCmax in monkey at 3 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698014 | Hepatic clearance in cynomolgus monkey administered through oral dosing | | | |
AID697684 | Ratio of free drug uptake in brain to plasma of Wistar rat at 100 mg/kg, po administered for 28 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697880 | Hypoglycemic activity in Goto-Kakizaki rat at 10 to 100 mg/kg, po dosed once daily for 28 days administered 60 mins before glucose challenge for 28 days by OGTT | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697635 | Intrinsic clearance in human liver microsomes | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697674 | Volume of distribution at steady state in monkey at 0.5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697876 | Hypoglycemic activity in normal Sprague-Dawley rat assessed as decrease in fasting glucose level at 100 mg/kg, po administered once daily for 28 days | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697640 | Drug uptake by human hepatic OATP1B3 transporter expressed in HEK293 cells relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697673 | Half life in monkey at 0.5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697885 | Antidiabetic activity in Wistar rat assessed as complete decrease in glycogen induced glucose excursion at 100 mg/kg, po administered as single dose 50 mins before glycogen challenge | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697682 | Ratio of free drug uptake in liver to plasma of Wistar rat at 100 mg/kg, po administered for 28 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697662 | fCmax in dog at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697634 | Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697672 | Clearance in monkey at 0.5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1059158 | Antidiabetic activity in Goto-Kakizaki rat diabetic model assessed as reduction in glucose excursion AUC at 100 mg/kg, po measured after 2 hrs by oral glucose tolerance test relative to control | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697637 | Activation of glucokinase in rat INS-1 cells assessed as stimulation of glucose-induced insulin secretion | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697657 | Half life in rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697639 | Drug uptake by human hepatic OATP1B1 transporter expressed in HEK293 cells relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697683 | Ratio of free drug uptake in pancreas to plasma of Wistar rat at 100 mg/kg, po administered for 28 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697636 | Apparent permeability across dog RRCK cells | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698013 | Ratio of drug level in human blood to plasma administered through oral dosing by LC-MS/MS analysis | | | |
AID697886 | Fraction unbound in Wistar rat brain at 50 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697884 | Antidiabetic activity in Wistar rat assessed as complete decrease in glycogen induced glucose excursion at 30 mg/kg, po administered as single dose 50 mins before glycogen challenge | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697667 | Oral bioavailability in dog at 5 mg/kg | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697675 | Oral bioavailability in monkey at 3 mg/kg | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697693 | Drug uptake in human hepatocytes in presence of pan OATP inhibitor rifamycin | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698011 | Fraction unbound in human plasma | | | |
AID697653 | fAUC (0 to 24 hrs) in rat at 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697883 | Antidiabetic activity in po dosed Wistar rat assessed as decrease in glycogen induced glucose excursion administered as single dose 50 mins before glycogen challenge | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697680 | Passive permeability across dog RRCK cells at pH 5.5 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697654 | fCmax in rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697665 | Half life in dog at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697656 | Clearance in rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697666 | Volume of distribution at steady state in dog at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697645 | Fraction unbound in human plasma at 50 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697862 | Drug uptake by rat hepatic OATP1A1 transporters expressed in CHO cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697874 | Antidiabetic activity in Goto-Kakizaki rat assessed as decrease in fasting plasma glucose level at 100 mg/kg, po administered once daily measured on day 14 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698004 | Fraction unbound in cynomolgus monkey plasma | | | |
AID697865 | Drug uptake by human hepatic OATP1B1 transporters expressed in HEK cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697881 | Antidiabetic activity in Goto-Kakizaki rat assessed as change in plasma insulin level at 10 to 100 mg/kg, po QD administered 60 mins before glucose challenge for 28 days by OGTT | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1698012 | Ratio of drug level in cynomolgus monkey blood to plasma administered through oral dosing by LC-MS/MS analysis | | | |
AID697870 | Activation of human hexokinase 3 at 500 times EC50 concentration | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697641 | Kinetic solubility of the compound | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697658 | Volume of distribution at steady state in rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697866 | Drug uptake by human hepatic OATP1B3 transporters expressed in HEK cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697864 | Drug uptake by rat hepatic OATP1B2 transporters expressed in CHO cells at 1 uM relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697691 | Drug uptake in human hepatocytes assessed per mg of protein | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1059151 | Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as total uptake | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697659 | Oral bioavailability in rat at 5 mg/kg | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697646 | Fraction unbound in rat liver at 1 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697689 | Ratio of free drug uptake in liver to pancreas of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697690 | Drug uptake in rat hepatocytes assessed per mg of protein | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697692 | Drug uptake in rat hepatocytes in presence of pan OATP inhibitor rifamycin | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1059154 | Apparent permeability in RRCK cells at pH 7.4 | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
AID697668 | fAUC (0 to 24 hrs) in monkey at 0.5 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697643 | Fraction unbound in dog plasma at 50 uM by equilibrium dialysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697655 | fCmax in rat at 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID697664 | Clearance in dog at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |