Assay Detail

CHEMBL3223989

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Binding

Induction of glucokinase translocation from nucleus to cytoplasm in rat hepatocytes in presence of 15 mM glucose

ChEMBL ↗

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Target

Hexokinase-4 (CHEMBL3882) ↗

Open DB target context

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Primary target Hexokinase-4

CHEMBL3882

Anchored from Assay target.

Protein identity Hexokinase-4

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Rattus norvegicus
Cell Type	Hepatocyte
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Hexokinase-4 (CHEMBL3882) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus

Pfefferkorn JA, Guzman-Perez A, Oates PJ, Litchfield J, Aspnes G, Basak A, Benbow J, Berliner MA, Bian J, Choi C, Freeman-Cook K, Corbett JW, Didiuk M, Dunetz JR, Filipski KJ, Hungerford WM, Jones CS, Karki K, Ling A, Li J, Patel L, Perreault C, Risley H, Saenz J, Song W, Tu M, Aiello R, Atkinson K, Barucci N, Beebe D, Bourassa P, Bourbounais F, Brodeur AM, Burbey R, Chen J, D'Aquila T, Derksen DR, Haddish-Berhane N, Huang C, Landro J, Lee Lapworth A, MacDougall M, Perregaux D, Pettersen J, Robertson A, Tan B, Treadway JL, Liu S, Qiu X, Knafels J, Ammirati M, Song X, DaSilva-Jardine P, Liras S, Sweet L, Rolph TP
Medchemcomm (2011) 2 : 828 -839
· DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	6.22	6.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2165615	NERIGLIATIN	2.0	1	6.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2165615	NERIGLIATIN	EC50	=	600.0	nM	6.22