Page last updated: 2024-11-13

pf-04991532

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID46181428
CHEMBL ID2165620
SCHEMBL ID1711504
MeSH IDM000602323

Synonyms (25)

Synonym
0h6 ,
6-({(2s)-3-cyclopentyl-2-[4-(trifluoromethyl)-1h-imidazol-1-yl]propanoyl}amino)pyridine-3-carboxylic acid
CHEMBL2165620 ,
pf-04991532
bdbm50394681
3-pyridinecarboxylic acid, 6-(((2s)-3-cyclopentyl-1-oxo-2-(4-(trifluoromethyl)-1h-imidazol-1-yl)propyl)amino)-
AJ212MS2O2 ,
1215197-37-7
pf 04991532
6-(3-cyclopentyl-2-(4-trifluoromethyl)-1h-imidazol-1-yl)propanamido)nicotinic acid
unii-aj212ms2o2
SCHEMBL1711504
6-[[(2s)-3-cyclopentyl-1-oxo-2-[4-(trifluoromethyl)-1h-imidazol-1-yl]propyl]amino]-3-pyridinecarboxylic acid
NCGC00485399-01
DB11765
HY-100181
CS-0018176
AKOS032962883
(s)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1h-imidazol-1-yl)propanamido)nicotinic acid
gkmlfbrlrvqvjo-zdusscgksa-n
(s)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1h-imidazol- 1-yl)propanamido)nicotinic acid
Q27273951
6-[[(2s)-3-cyclopentyl-2-[4-(trifluoromethyl)imidazol-1-yl]propanoyl]amino]pyridine-3-carboxylic acid
MS-26673
BP168016

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hexokinase-4 Rattus norvegicus (Norway rat)EC50 (µMol)3.54500.19002.66336.9000AID697637; AID697871
Hexokinase-4Homo sapiens (human)EC50 (µMol)0.09000.09001.26876.3200AID697634
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
glucose catabolic processHexokinase-4Homo sapiens (human)
regulation of glycolytic processHexokinase-4Homo sapiens (human)
NADP metabolic processHexokinase-4Homo sapiens (human)
response to glucoseHexokinase-4Homo sapiens (human)
positive regulation of insulin secretionHexokinase-4Homo sapiens (human)
cellular response to insulin stimulusHexokinase-4Homo sapiens (human)
glucose homeostasisHexokinase-4Homo sapiens (human)
regulation of potassium ion transportHexokinase-4Homo sapiens (human)
cellular response to leptin stimulusHexokinase-4Homo sapiens (human)
negative regulation of gluconeogenesisHexokinase-4Homo sapiens (human)
positive regulation of glycogen biosynthetic processHexokinase-4Homo sapiens (human)
regulation of insulin secretionHexokinase-4Homo sapiens (human)
glucose 6-phosphate metabolic processHexokinase-4Homo sapiens (human)
canonical glycolysisHexokinase-4Homo sapiens (human)
calcium ion importHexokinase-4Homo sapiens (human)
glucose metabolic processHexokinase-4Homo sapiens (human)
intracellular glucose homeostasisHexokinase-4Homo sapiens (human)
glycolytic processHexokinase-4Homo sapiens (human)
carbohydrate phosphorylationHexokinase-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
glucokinase activityHexokinase-4Homo sapiens (human)
protein bindingHexokinase-4Homo sapiens (human)
ATP bindingHexokinase-4Homo sapiens (human)
glucose bindingHexokinase-4Homo sapiens (human)
glucose sensor activityHexokinase-4Homo sapiens (human)
fructokinase activityHexokinase-4Homo sapiens (human)
mannokinase activityHexokinase-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
nucleoplasmHexokinase-4Homo sapiens (human)
cytosolHexokinase-4Homo sapiens (human)
mitochondrionHexokinase-4Homo sapiens (human)
cytosolHexokinase-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (105)

Assay IDTitleYearJournalArticle
AID697663fCmax in dog at 5 mg/kg, po2012Journal 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.
AID697648Fraction unbound in rat pancreas at 1 uM by equilibrium dialysis2012Journal 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.
AID697868Activation of human hexokinase 1 at 500 times EC50 concentration2012Journal 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.
AID697875Antidiabetic activity in Goto-Kakizaki rat assessed as decrease in fasting plasma glucose level at 100 mg/kg, po administered once daily measured on day 282012Journal 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.
AID697676Drug excretion in rat bile2012Journal 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.
AID697863Drug uptake by rat hepatic OATP1A4 transporters expressed in CHO cells at 1 uM relative to control2012Journal 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.
AID697660fAUC (0 to 24 hrs) in dog at 1 mg/kg, iv2012Journal 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.
AID697677Renal excretion in rat2012Journal 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.
AID697678Fraction absorbed in portal vein cannulated rat at 5 mg/kg, iv2012Journal 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.
AID697649Fraction unbound in dog pancreas at 1 uM by equilibrium dialysis2012Journal 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.
AID697670fCmax in monkey at 0.5 mg/kg, iv2012Journal 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.
AID697882Antidiabetic 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 OGTT2012Journal 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.
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1059152Apparent permeability in RRCK cells at pH 5.52013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697647Fraction unbound in dog liver at 1 uM by equilibrium dialysis2012Journal 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.
AID1059149Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as active uptake2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697669fAUC (0 to 24 hrs) in monkey at 3 mg/kg, po2012Journal 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.
AID697686Ratio of free drug uptake in liver to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing2012Journal 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.
AID697879Antidiabetic 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 OGTT2012Journal 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.
AID697679Thermodynamic solubility of the compound at pH 6.52012Journal 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.
AID697681Passive permeability across dog RRCK cells at pH 7.42012Journal 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.
AID697878Antidiabetic 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 OGTT2012Journal 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.
AID697685Ratio 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 dosing2012Journal 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.
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID1059153Apparent permeability in RRCK cells at pH 6.52013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID1059150Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as passive uptake2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697661fAUC (0 to 24 hrs) in dog at 5 mg/kg, po2012Journal 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.
AID697688Ratio of free drug uptake in brain to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing2012Journal 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.
AID697869Activation of human hexokinase 2 at 500 times EC50 concentration2012Journal 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.
AID697867Drug uptake by human hepatic OATP2B1 transporters expressed in HEK cells at 1 uM relative to control2012Journal 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.
AID697871Induction of glucokinase translocation from nucleus to cytoplasm in cryopreserved rat hepatocytes after 1 hr by Hoechst staining-based fluorescence microscopic analysis2012Journal 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.
AID697642Fraction unbound in rat plasma at 50 uM by equilibrium dialysis2012Journal 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.
AID1698015Hepatic clearance in human administered through oral dosing
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID1059183Lipophilicity, log D of the compound at pH 7.42013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697651Fraction unbound in dog brain at 1 uM by equilibrium dialysis2012Journal 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.
AID697687Ratio of free drug uptake in pancreas to plasma of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing2012Journal 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.
AID697650Fraction unbound in rat brain at 1 uM by equilibrium dialysis2012Journal 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.
AID697644Fraction unbound in monkey plasma at 50 uM by equilibrium dialysis2012Journal 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.
AID697873Activation 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 immunoassay2012Journal 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.
AID697652fAUC (0 to 24 hrs) in rat at 1 mg/kg, iv2012Journal 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.
AID697638Ratio of EC50 for activation of glucokinase in rat INS-1 cells to EC50 for in-vitro activation of rat glucokinase2012Journal 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.
AID697671fCmax in monkey at 3 mg/kg, po2012Journal 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.
AID1698014Hepatic clearance in cynomolgus monkey administered through oral dosing
AID697684Ratio 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 dosing2012Journal 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.
AID697880Hypoglycemic 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 OGTT2012Journal 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.
AID697635Intrinsic clearance in human liver microsomes2012Journal 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.
AID697674Volume of distribution at steady state in monkey at 0.5 mg/kg, iv2012Journal 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.
AID697876Hypoglycemic activity in normal Sprague-Dawley rat assessed as decrease in fasting glucose level at 100 mg/kg, po administered once daily for 28 days2012Journal 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.
AID697640Drug uptake by human hepatic OATP1B3 transporter expressed in HEK293 cells relative to control2012Journal 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.
AID697673Half life in monkey at 0.5 mg/kg, iv2012Journal 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.
AID697885Antidiabetic 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 challenge2012Journal 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.
AID697682Ratio 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 dosing2012Journal 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.
AID697662fCmax in dog at 1 mg/kg, iv2012Journal 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.
AID697634Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometric analysis2012Journal 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.
AID697672Clearance in monkey at 0.5 mg/kg, iv2012Journal 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.
AID1059158Antidiabetic 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 control2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697637Activation of glucokinase in rat INS-1 cells assessed as stimulation of glucose-induced insulin secretion2012Journal 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.
AID697657Half life in rat at 1 mg/kg, iv2012Journal 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.
AID697639Drug uptake by human hepatic OATP1B1 transporter expressed in HEK293 cells relative to control2012Journal 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.
AID697683Ratio 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 dosing2012Journal 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.
AID697636Apparent permeability across dog RRCK cells2012Journal 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.
AID1698013Ratio of drug level in human blood to plasma administered through oral dosing by LC-MS/MS analysis
AID697886Fraction unbound in Wistar rat brain at 50 mg/kg, po2012Journal 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.
AID697884Antidiabetic 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 challenge2012Journal 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.
AID697667Oral bioavailability in dog at 5 mg/kg2012Journal 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.
AID697675Oral bioavailability in monkey at 3 mg/kg2012Journal 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.
AID697693Drug uptake in human hepatocytes in presence of pan OATP inhibitor rifamycin2012Journal 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.
AID1698011Fraction unbound in human plasma
AID697653fAUC (0 to 24 hrs) in rat at 5 mg/kg, po2012Journal 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.
AID697883Antidiabetic activity in po dosed Wistar rat assessed as decrease in glycogen induced glucose excursion administered as single dose 50 mins before glycogen challenge2012Journal 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.
AID697680Passive permeability across dog RRCK cells at pH 5.52012Journal 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.
AID697654fCmax in rat at 1 mg/kg, iv2012Journal 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.
AID697665Half life in dog at 1 mg/kg, iv2012Journal 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.
AID697656Clearance in rat at 1 mg/kg, iv2012Journal 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.
AID697666Volume of distribution at steady state in dog at 1 mg/kg, iv2012Journal 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.
AID697645Fraction unbound in human plasma at 50 uM by equilibrium dialysis2012Journal 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.
AID697862Drug uptake by rat hepatic OATP1A1 transporters expressed in CHO cells at 1 uM relative to control2012Journal 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.
AID697874Antidiabetic activity in Goto-Kakizaki rat assessed as decrease in fasting plasma glucose level at 100 mg/kg, po administered once daily measured on day 142012Journal 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.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID697865Drug uptake by human hepatic OATP1B1 transporters expressed in HEK cells at 1 uM relative to control2012Journal 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.
AID697881Antidiabetic 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 OGTT2012Journal 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.
AID1698012Ratio of drug level in cynomolgus monkey blood to plasma administered through oral dosing by LC-MS/MS analysis
AID697870Activation of human hexokinase 3 at 500 times EC50 concentration2012Journal 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.
AID697641Kinetic solubility of the compound2012Journal 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.
AID697658Volume of distribution at steady state in rat at 1 mg/kg, iv2012Journal 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.
AID697866Drug uptake by human hepatic OATP1B3 transporters expressed in HEK cells at 1 uM relative to control2012Journal 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.
AID697864Drug uptake by rat hepatic OATP1B2 transporters expressed in CHO cells at 1 uM relative to control2012Journal 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.
AID697691Drug uptake in human hepatocytes assessed per mg of protein2012Journal 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.
AID1059151Organic anion transporter-mediated drug uptake in rat hepatocytes assessed as total uptake2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697659Oral bioavailability in rat at 5 mg/kg2012Journal 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.
AID697646Fraction unbound in rat liver at 1 uM by equilibrium dialysis2012Journal 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.
AID697689Ratio of free drug uptake in liver to pancreas of dog at 50 mg/kg, po administered for 4 days measured 4 hrs post last dosing2012Journal 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.
AID697690Drug uptake in rat hepatocytes assessed per mg of protein2012Journal 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.
AID697692Drug uptake in rat hepatocytes in presence of pan OATP inhibitor rifamycin2012Journal 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.
AID1059154Apparent permeability in RRCK cells at pH 7.42013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
AID697668fAUC (0 to 24 hrs) in monkey at 0.5 mg/kg, iv2012Journal 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.
AID697643Fraction unbound in dog plasma at 50 uM by equilibrium dialysis2012Journal 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.
AID697655fCmax in rat at 5 mg/kg, po2012Journal 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.
AID697664Clearance in dog at 1 mg/kg, iv2012Journal 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (50.00)24.3611
2020's3 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.74 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]