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PDBsum entry 2c68
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References listed in PDB file
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Key reference
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Title
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Triazolo[1,5-A]pyrimidines as novel cdk2 inhibitors: protein structure-Guided design and sar.
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Authors
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C.M.Richardson,
D.S.Williamson,
M.J.Parratt,
J.Borgognoni,
A.D.Cansfield,
P.Dokurno,
G.L.Francis,
R.Howes,
J.D.Moore,
J.B.Murray,
A.Robertson,
A.E.Surgenor,
C.J.Torrance.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
1353-1357.
[DOI no: ]
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PubMed id
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Abstract
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Crystallographic and modelling data, in conjunction with a medicinal chemistry
template-hopping approach, led to the identification of a series of novel and
potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity
over glycogen synthase kinase-3beta (GSK-3beta). One example had a CDK2 IC(50)
of 120 nM and showed selectivity over GSK-3beta of 167-fold.
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