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Target not currently curated in GtoImmuPdb

Target id: 2798

Nomenclature: Glucokinase

Family: Hexokinases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 465 7p13 GCK glucokinase
Mouse - 465 11 3.88 cM Gck glucokinase
Rat - 465 14q21 Gck glucokinase
Gene and Protein Information Comments
In humans, the 465 amino acid form (isoform 1, NM_000162) is expressed specifically in pancreatic β cells. Isoforms 2 (466 amino acids, NM_NM_033507) and 3 (464 amino acids, NM_033508) are expressed in the liver, with isoform 2 being the predominant hepatic variant. The mouse expresses two isoforms; isoform 1 (465 amino acids, NM_010292) in pancreatic β cells and isoform 2 (465 amino acids, NM_001287386) in the liver.
Previous and Unofficial Names Click here for help
glucokinase (hexokinase 4)
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AZD1656 Small molecule or natural product Primary target of this compound Hs Activation 7.2 pEC50 1
pEC50 7.2 (EC50 5.7x10-8 M) [1]
BMS-820132 Small molecule or natural product Ligand has a PDB structure Hs Activation - - 2
Description: Partial activation AC50= 29 nM, maximal enzyme activation (Ymax)- 143%
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
dorzagliatin Small molecule or natural product Approved drug Hs Activation - - 3
Description: Full activator
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Diabetes mellitus, noninsulin-dependent; NIDDM
Synonyms: Diabetes mellitus, Type II; T2D [OMIM: 125853]
Maturity onset diabetes
Type 2 diabetes mellitus [Disease Ontology: DOID:9352]
Disease Ontology: DOID:9352
OMIM: 125853
Disease:  Diabetes mellitus, permanent neonatal; PNDM
Synonyms: DEND syndrome [Orphanet: ORPHA79134]
Developmental delay-epilepsy-neonatal diabetes syndrome [Orphanet: ORPHA79134]
Permanent neonatal diabetes mellitus [Orphanet: ORPHA99885]
OMIM: 606176
Orphanet: ORPHA99885, ORPHA79134
Disease:  Hyperinsulinemic hypoglycemia, familial, 3; HHF3
Synonyms: Hyperinsulinemic hypoglycemia [Disease Ontology: DOID:13317]
Hyperinsulinism due to glucokinase deficiency [Orphanet: ORPHA79299]
Disease Ontology: DOID:13317
OMIM: 602485
Orphanet: ORPHA79299
Disease:  Maturity-onset diabetes of the young, type 2; MODY2
Synonyms: Maturity-onset diabetes of the young [Orphanet: ORPHA552] [OMIM: 606391] [Disease Ontology: DOID:0050524]
MODY [Orphanet: ORPHA552] [OMIM: 606391]
Disease Ontology: DOID:0050524
OMIM: 125851, 606391
Orphanet: ORPHA552


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1. AstraZeneca. AZD1656. Accessed on 17/09/2014. Modified on 17/09/2014.,

2. Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S et al.. (2022) Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132). J Med Chem, 65 (5): 4291-4317. [PMID:35179904]

3. Wang P, Liu H, Chen L, Duan Y, Chen Q, Xi S. (2017) Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res, 2017: 5812607. [PMID:28191470]

How to cite this page

Hexokinases: Glucokinase. Last modified on 09/08/2022. Accessed on 19/06/2024. IUPHAR/BPS Guide to PHARMACOLOGY,