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Paul D. Eve

Institute of Cancer Research

18

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465

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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

2019 European Journal of Medicinal Chemistry
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Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)

2016 Journal of Medicinal Chemistry
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AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

2012 Clinical Cancer Research
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Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.

2012 Journal of Medicinal Chemistry
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Structure of PKA-PKB chimera complexed with (1S)-2-amino-1-(4- chlorophenyl)-1-(4-(1H-pyrazol-4-yl)phenyl)ethan-1-ol

2012
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CCT244747 is a novel, potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs

2012 Clinical Cancer Research
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Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

2011 Journal of Medicinal Chemistry
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CCT241533 Is a Potent and Selective Inhibitor of CHK2 that Potentiates the Cytotoxicity of PARP Inhibitors

2011 Cancer Research
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Abstract A235: Structure-guided evolution of potent and selective oral inhibitors of CHK1 through scaffold morphing.

2011 Molecular Cancer Therapeutics
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Abstract 4481: First report of preclinical pharmacology of two novel potent AKT inhibitors and development of pharmacodynamic (PD) biomarkers in tumor and surrogate tissue

2010 Cancer Research
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