G W. Aherne

London, ENG, United Kingdom

Last Updated: 09/26/2026

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Found 8 publications

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).

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).

Journal: Journal of medicinal chemistry
Published: May 12, 2016

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.

Journal: Oncotarget
Published: April 30, 2015

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

Journal: Oncotarget
Published: September 28, 2013

Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Journal: PloS one
Published: November 23, 2012

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

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

Journal: Journal of medicinal chemistry
Published: October 23, 2012

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

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

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research
Published: August 30, 2012

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.

Journal: Journal of medicinal chemistry
Published: March 13, 2012

Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.

Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.

Journal: Journal of medicinal chemistry
Published: November 25, 2011
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Last Updated: 09/26/2026