Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1<i>H</i>-indol-5-yl)-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Jeffrey M. Axten, Jesús R. Medina, Yanhong Feng, +21

Journal of Medicinal Chemistry

Chemoprevention StrategyChemical BiologyPharmaceutical ChemistryTumor BiologyMolecular Pharmacology +22

Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity

Charity Atkins, Qi Liu, Elisabeth A. Minthorn, +12

Cancer Research

Tumor BiologySignaling PathwayUpr SignalingCell RegulationReceptor Tyrosine Kinase +19

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

Jeffrey M. Axten, Stuart P. Romeril, Arthur Y. L. Shu, +15

ACS Medicinal Chemistry Letters

Drug Discovery ProgramTumor BiologyPhysical PropertiesMedicinal ChemistrySignaling Pathway +16

GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers

Peter Sabbatini, Susan Korenchuk, Jason L. Rowand, +17

Molecular Cancer Therapeutics

Antitumor ActivityImmunologyGlucose HomeostasisExperimental ModelsInsulin Receptor +14

Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase

Peter Sabbatini, Jason L. Rowand, Arthur Groy, +10

Clinical Cancer Research

&lt;i&gt;In vitro&lt;/i&gt; and &lt;i&gt;in vivo&lt;/i&gt; induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor

Aidan G. Gilmartin, Arthur Groy, Elizabeth R. Gore, +20

Haematologica

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

Stanley D. Chamberlain, Anikó M. Redman, Joseph W. Wilson, +18

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryNatural SciencesMedicineReceptor Tyrosine Kinase +6

In Vivo Cardiac Electrophysiologic Effects of a Novel Diphenylphosphine Oxide IKur Blocker, (2-Isopropyl-5-methylcyclohexyl) Diphenylphosphine Oxide, in Rat and Nonhuman Primate

Christopher P. Regan, Audrey A. Wallace, Hillary K. Cresswell, +2

Journal of Pharmacology and Experimental Therapeutics

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

Kyle A. Emmitte, Brian J. Wilson, Erich W. Baum, +22

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryNatural SciencesMedicineRational Drug Design +5

Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase

Stanley D. Chamberlain, Joseph W. Wilson, Felix Deanda, +17

Bioorganic & Medicinal Chemistry Letters

BiochemistryMedicineNatural SciencesReceptor Tyrosine KinaseRational Drug Design +6