Assay Detail

CHEMBL3749779

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Binding

Inhibition of GSK3beta (unknown origin)

ChEMBL ↗

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Target

Glycogen synthase kinase-3 beta (CHEMBL262) ↗

Open DB target context

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Glycogen synthase kinase-3 beta (CHEMBL262) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Glycogen synthase kinase-3 beta

CHEMBL262

Anchored from Assay target.

Protein identity Glycogen synthase kinase-3 beta

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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Glycogen synthase kinase-3 beta (CHEMBL262) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.

Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M, Muller K, Bellamacina C, Lindvall MK, Zang R, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Basham S, Chan J, Ginn E, Aycinena A, Holash J, Castillo J, Langowski JL, Wang Y, Chen MY, Lambert A, Fritsch C, Kauffmann A, Pfister E, Vanasse KG, Garcia PD.
J Med Chem (2015) 58 : 8373 -8386
PubMed 26505898 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	5.89	5.89

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3651966	LGH-447	1.0	1	5.89

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3651966	LGH-447	IC50	=	1300.0	nM	5.89