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Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK)

Journal of medicinal chemistry, 2016-08, Vol.59 (16), p.7478-7496

2016

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Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2

The Journal of immunology (1950), 2011-10, Vol.187 (7), p.3840-3853

2011

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A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis

Arthritis research & therapy, 2011-04, Vol.13 (2), p.R68-R68

2011

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Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors

Expert opinion on drug discovery, 2016-12, Vol.11 (12), p.1187-1199

2016

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Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase

Journal of medicinal chemistry, 2012-05, Vol.55 (10), p.4580-4593

2012

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Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells

Blood, 2006-02, Vol.107 (4), p.1617-1623

2006

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Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis

Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (8), p.2158-2162

2006

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Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors

Journal of medicinal chemistry, 2012-01, Vol.55 (1), p.115-125

2012

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ALK Mutants in the Kinase Domain Exhibit Altered Kinase Activity and Differential Sensitivity to Small Molecule ALK Inhibitors

Biochemistry (Easton), 2009-04, Vol.48 (16), p.3600-3609

2009

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Synthesis and Mixed Lineage Kinase Activity of Pyrrolocarbazole and Isoindolone Analogs of (+)K-252a

Journal of medicinal chemistry, 2007-02, Vol.50 (3), p.433-441

2007

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Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test

Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (3), p.1421-1426

2012

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CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers

Molecular cancer therapeutics, 2012-03, Vol.11 (3), p.670-679

2012

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A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779

Journal of medicinal chemistry, 2012-06, Vol.55 (11), p.5243-5254

2012

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Neurotrophic 3,9-Bis[(alkylthio)methyl]- and -Bis(alkoxymethyl)-K-252a Derivatives

Journal of medicinal chemistry, 1997-06, Vol.40 (12), p.1863-1869

1997

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1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (6), p.1793-1798

2007

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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase

Bioorganic & medicinal chemistry letters, 2015-03, Vol.25 (5), p.1047-1052

2015

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Phosphoregulation of Mixed-Lineage Kinase 1 Activity by Multiple Phosphorylation in the Activation Loop

Biochemistry (Easton), 2004-12, Vol.43 (51), p.16348-16355

2004

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2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity

Journal of medicinal chemistry, 2011-09, Vol.54 (18), p.6328-6341

2011

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Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group

Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (24), p.7261-7264

2011

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TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (12), p.3551-3555

2008

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Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.463-466

2011

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Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3- b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase

Bioorganic & medicinal chemistry, 2010-06, Vol.18 (12), p.4351-4362

2010

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A Cellular Assay for Inhibitors of the Fatty Acid Biosynthetic Pathway Using Scintillating Microplates

Assay and drug development technologies, 2015-06, Vol.13 (5), p.285

2015

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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors

Bioorganic & medicinal chemistry letters, 2011-07, Vol.21 (13), p.3877-3880

2011

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Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK)

Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis

Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors

Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase

Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells

Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis

Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors

ALK Mutants in the Kinase Domain Exhibit Altered Kinase Activity and Differential Sensitivity to Small Molecule ALK Inhibitors

Synthesis and Mixed Lineage Kinase Activity of Pyrrolocarbazole and Isoindolone Analogs of (+)K-252a

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test

CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers

A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779

Neurotrophic 3,9-Bis[(alkylthio)methyl]- and -Bis(alkoxymethyl)-K-252a Derivatives

1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase

Phosphoregulation of Mixed-Lineage Kinase 1 Activity by Multiple Phosphorylation in the Activation Loop

2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity

Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group

TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone

Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models

Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3- b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase

A Cellular Assay for Inhibitors of the Fatty Acid Biosynthetic Pathway Using Scintillating Microplates

Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors

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