Identification of 4-(4-Aminopiperidin-1-yl)-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidines as Selective Inhibitors of Protein Kinase B through Fragment Elaboration

John Caldwell, Thomas G. Davies, Alastair Donald, +11

Journal of Medicinal Chemistry

A Structural Comparison of Inhibitor Binding to PKB, PKA and PKA-PKB Chimera

Thomas G. Davies, Marcel L. Verdonk, Brent Graham, +9

Journal of Molecular Biology

BiochemistryPka-pkb ChimeraNatural SciencesMedicineMechanism Of Action +9

Discovery of 4-Amino-1-(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)piperidine-4-carboxamides As Selective, Orally Active Inhibitors of Protein Kinase B (Akt)

Tatiana McHardy, John Caldwell, Kwai-Ming J. Cheung, +15

Journal of Medicinal Chemistry

Drug TargetRelated Kinase PkaPharmacotherapyChemical BiologyPharmaceutical Chemistry +15

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

Mike I. Walton, Paul D. Eve, Angela Hayes, +19

Oncotarget

ImmunologyPs296 Chk1PathologyCell DeathCancer Biology +17

Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design

Alastair Donald, Tatiana McHardy, Martin Rowlands, +7

Journal of Medicinal Chemistry

Molecular mechanisms of human IRE1 activation through dimerization and ligand binding

Amar Joshi, Yvette Newbatt, Craig McAndrew, +8

Oncotarget

Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening

Thomas P. Matthews, Suki Klair, Samantha Burns, +13

Journal of Medicinal Chemistry

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (<i>R</i>)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)

James Osborne, Thomas P. Matthews, Tatiana McHardy, +24

Journal of Medicinal Chemistry

Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors

Michael Lainchbury, Thomas P. Matthews, Tatiana McHardy, +13

Journal of Medicinal Chemistry

Tumor BiologyMedicinal ChemistryLead ScaffoldsBiochemistryCheckpoint Kinase 1 +11

Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases

Thomas P. Matthews, Tatiana McHardy, Suki Klair, +12

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryHealth SciencesMedicineRational Drug DesignAnti-cancer Agent +6