The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28284804 |
56 |
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. |
Merck |
26985301 |
55 |
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors. |
Glaxosmithkline |
26685731 |
33 |
Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. |
Servier Research Institute of Medicinal Chemistry |
25815149 |
24 |
Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM. |
Yuhan Research Institute |
25001129 |
89 |
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. |
Amgen |
25516785 |
26 |
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators. |
Amgen |
25203462 |
49 |
Discovery of 2-pyridylureas as glucokinase activators. |
Array Biopharma |
24588963 |
21 |
Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H-pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. |
Yuhan Research Institute |
24583379 |
2 |
Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPAR¿. |
Chinese Academy of Medical Sciences & Peking Union Medical College |
24405172 |
35 |
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. |
Amgen |
24405213 |
60 |
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. |
Amgen |
24239482 |
9 |
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
Pfizer |
24015910 |
18 |
Identification of a new class of glucokinase activators through structure-based design. |
Array Biopharma |
23831135 |
29 |
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. |
Pfizer |
24294411 |
3 |
Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose. |
Florida State University |
23434031 |
51 |
Design, synthesis and SAR of novel glucokinase activators. |
Takeda California |
23218712 |
29 |
Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. |
Yuhan Research Institute |
23149230 |
22 |
The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. |
Astrazeneca |
23089526 |
21 |
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus. |
Pfizer |
22196621 |
17 |
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. |
Pfizer |
22459213 |
29 |
Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. |
Chinese Academy of Sciences |
19435665 |
33 |
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. |
Pfizer |
21515051 |
23 |
Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. |
Astrazeneca R&D |
20472448 |
25 |
Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. |
Chinese Academy of Sciences |
19736020 |
32 |
The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. |
Banyu Tsukuba Research Institute |
19726182 |
60 |
Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. |
Banyu Tsukuba Research Institute |
19540111 |
24 |
Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. |
Banyu Tsukuba Research Institute |
19427223 |
68 |
Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. |
Banyu Tsukuba Research Institute |
19362831 |
11 |
Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. |
Banyu Tsukuba Research Institute |
19282189 |
50 |
Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. |
Banyu Tsukuba Research Institute |
19188063 |
66 |
Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. |
Banyu Tsukuba Research Institute |
18588279 |
13 |
SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1. |
(Osi) Prosidion |
16503142 |
6 |
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. |
Astrazeneca R&D |
15808477 |
23 |
Discovery, synthesis and biological evaluation of novel glucokinase activators. |
Astrazeneca |
32527453 |
16 |
Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. |
Chiba University |
31818630 |
41 |
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. |
Array Biopharma |
27391254 |
7 |
Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times. |
Istituto Italiano Di Tecnologia |
27437083 |
94 |
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. |
Amgen |
27437074 |
100 |
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. |
Amgen |
31693351 |
473 |
Discovery of 4 |
TBA |
30600148 |
65 |
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors. |
Zhejiang University |
30384048 |
365 |
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
University of Florida |
26551034 |
82 |
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N ? S (nN ? ?*S-X) Interaction for Conformational Constraint. |
Amgen |
28800453 |
51 |
Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. |
China Pharmaceutical University |
28512030 |
26 |
Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. |
Takeda California |
28284809 |
7 |
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. |
Merck |
11179435 |
15 |
Discovery of a novel member of the histamine receptor family. |
The Centre For Addiction and Mental Health |