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Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544

Organic process research & development, 2012-01, Vol.16 (1), p.70-81

2012

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Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells: metabolic basis and potential clinical implications

The Journal of biological chemistry, 2013-02, Vol.288 (5), p.3500-3511

2013

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Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model

BMC genomics, 2008-06, Vol.9 (1), p.264-264, Article 264

2008

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Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration

Molecular cancer therapeutics, 2017-12, Vol.16 (12), p.2677-2688

2017

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Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1887-1891

2018

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The development of potent and selective bisarylmaleimide GSK3 inhibitors

Bioorganic & medicinal chemistry letters, 2005-02, Vol.15 (4), p.899-903

2005

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Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (7), p.1377-1380

2015

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Pharmacological Inhibition of Nicotinamide Phosphoribosyltransferase (NAMPT), an Enzyme Essential for NAD+ Biosynthesis, in Human Cancer Cells

The Journal of biological chemistry, 2013-02, Vol.288 (5), p.3500-3511

2013

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Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics

Cancer management and research, 2011, Vol.3, p.157-175

2011

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Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics

Cancer management and research, 2011-05, Vol.3 (default), p.157-175

2011

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Abstract 3042: LY2801653: An orally bioavailable MET kinase inhibitor with inhibitory activity against the oncoproteins ROS1 and MKNK1/2

Cancer research (Chicago, Ill.), 2013-04, Vol.73 (8_Supplement), p.3042-3042

2013

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Abstract 2820: LY2784544, a small molecule JAK2 inhibitor, induces apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.2820-2820

2011

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Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models

Blood, 2010-11, Vol.116 (21), p.4087-4087

2010

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Synthesis and SAR of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/Tachykinin NK1 receptor antagonist activity

Bioorganic & medicinal chemistry letters, 1997-11, Vol.7 (22), p.2819-2824

1997

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An acyliminium ion route to [formula omitted] and [formula omitted] “Anti” phe-gly dipeptide mimetics

Bioorganic & medicinal chemistry letters, 1991, Vol.1 (6), p.309-312

1991

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Effect of MDL 105,212, a nonpeptide NK-1/NK-2 receptor antagonist in an allergic guinea pig model

The Journal of pharmacology and experimental therapeutics, 1996-11, Vol.279 (2), p.732

1996

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In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist

The Journal of pharmacology and experimental therapeutics, 1996-05, Vol.277 (2), p.840

1996

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Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors

Bioorganic & medicinal chemistry letters, 1996-04, Vol.6 (8), p.951-956

1996

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Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists

Bioorganic & medicinal chemistry letters, 1997-10, Vol.7 (19), p.2531-2536

1997

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Synthesis of 6-amino-5-oxo-7-phenyl-1,4-oxazepines as conformationally constrained gauche (−) dipeptide mimetics

Bioorganic & medicinal chemistry letters, 1993-02, Vol.3 (2), p.231-234

1993

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Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK 1 and NK 2 receptors

Bioorganic & medicinal chemistry letters, 1996, Vol.6 (8), p.951-956

1996

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Synthesis and sar of 4-(1 H-benzimidazole-2-carbonyl)piperidines with dual histamine H 1/tachykinin NK 1 receptor antagonist activity

Bioorganic & medicinal chemistry letters, 1997, Vol.7 (22), p.2819-2824

1997

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Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544

Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells: metabolic basis and potential clinical implications

Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3

Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model

Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration

Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT

The development of potent and selective bisarylmaleimide GSK3 inhibitors

Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists

Pharmacological Inhibition of Nicotinamide Phosphoribosyltransferase (NAMPT), an Enzyme Essential for NAD+ Biosynthesis, in Human Cancer Cells

Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model

Erratum to: Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model

Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics

Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics

Abstract 3042: LY2801653: An orally bioavailable MET kinase inhibitor with inhibitory activity against the oncoproteins ROS1 and MKNK1/2

Abstract 2820: LY2784544, a small molecule JAK2 inhibitor, induces apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway

Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models

Synthesis and SAR of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/Tachykinin NK1 receptor antagonist activity

An acyliminium ion route to [formula omitted] and [formula omitted] “Anti” phe-gly dipeptide mimetics

Effect of MDL 105,212, a nonpeptide NK-1/NK-2 receptor antagonist in an allergic guinea pig model

In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist

Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors

Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists

Synthesis of 6-amino-5-oxo-7-phenyl-1,4-oxazepines as conformationally constrained gauche (−) dipeptide mimetics

Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK 1 and NK 2 receptors

Synthesis and sar of 4-(1 H-benzimidazole-2-carbonyl)piperidines with dual histamine H 1/tachykinin NK 1 receptor antagonist activity

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