3q3b

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6-Amino-4-(pyrimidin-4-yl)pyridones: Novel Glycogen Synthase Kinase-3 Inhibitors6-Amino-4-(pyrimidin-4-yl)pyridones: Novel Glycogen Synthase Kinase-3 Inhibitors

Structural highlights

3q3b is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Gene:GSK3B (Homo sapiens)
Activity:[Tau_protein_kinase [Tau protein] kinase], with EC number 2.7.11.26
Resources:FirstGlance, OCA, RCSB, PDBsum

Publication Abstract from PubMed

The synthesis and structure-activity relationships for a novel series of 6-amino-4-(pyrimidin-4-yl)pyridones derived from a high throughput screening hit are discussed. Optimization of lead matter afforded compounds with good potency, selectivity and central nervous system (CNS) exposure.

6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3beta inhibitors.,Coffman K, Brodney M, Cook J, Lanyon L, Pandit J, Sakya S, Schachter J, Tseng-Lovering E, Wessel M Bioorg Med Chem Lett. 2011 Mar 1;21(5):1429-33. Epub 2011 Jan 11. PMID:21295469[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

See Also

References

  1. Coffman K, Brodney M, Cook J, Lanyon L, Pandit J, Sakya S, Schachter J, Tseng-Lovering E, Wessel M. 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3beta inhibitors. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1429-33. Epub 2011 Jan 11. PMID:21295469 doi:10.1016/j.bmcl.2011.01.017

3q3b, resolution 2.70Å

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