| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID697872 | Activation of glucokinase in Sprague-Dawley rat islets assessed as enhancement of glucose-stimulated insulin secretion 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. |
| AID1378921 | Activation of recombinant human liver glucokinase 2 assessed as assessed as reduction in Km for glucose in presence of 5 mM glucose by G6PDH coupled assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378927 | Toxicity in db/db mouse BKS.Cg-Dock7m+/+ Leprdb/J assessed as dyslipidemia by measuring increase in cholesterol level at 25 mg/kg, po administered daily for 5 weeks | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378916 | Activation of recombinant human liver glucokinase 2 assessed as reduction in NADH production in presence of 5 mM glucose by G6PDH coupled assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378919 | Cytoprotection in rat INS1(832/13) cells assessed as reduction in streptozocin induced beta cells apoptosis after 20 hrs by MTT based spectrophotometric method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| 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. |
| 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. |
| AID762301 | Activation of human recombinant glucokinase assessed as ratio of the glucokinase Km at maximum compound concentration to the enzyme Km in the absence of compound | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
| Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. |
| 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. |
| AID1378918 | Activation of glucokinase in rat INS1(832/13) cells assessed as increase in glucose sensitive insulin secretion at 20 uM after 2 hrs in presence of 5.5 mM glucose by AlphaLISA method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378928 | Toxicity in db/db mouse BKS.Cg-Dock7m+/+ Leprdb/J assessed as dyslipidemia by measuring increase in low density lipoprotein-cholesterol level at 25 mg/kg, po administered daily for 5 weeks | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378920 | Cytoprotection in rat INS1(832/13) cells assessed as reduction in streptozocin induced beta cells apoptosis after 20 hrs by MTT based spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID1378917 | Increase in glucose uptake in mouse primary hepatocytes assessed as glucose uptake level at 20 uM after 24 hrs by glucose oxidase method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| 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. |
| AID1378915 | Activation of recombinant human liver glucokinase 2 assessed as reduction in NADH production in presence of 5 mM glucose by G6PDH coupled assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
| AID762300 | Activation of human recombinant glucokinase assessed as ratio of the enzyme velocity at maximum compound concentration to the enzyme Km in the absence of compound | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
| Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. |
| 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. |
| 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. |
| AID762302 | Activation of human recombinant glucokinase by matrix assay in presence of glucose | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
| Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |