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Knowledge Based Prediction of Ligand Binding Modes and Rational Inhibitor Design for Kinase Drug Discovery

Journal of medicinal chemistry, 2008-09, Vol.51 (17), p.5149-5171

2008

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Discovery of a Potent, Selective, and Orally Active Proteasome Inhibitor for the Treatment of Cancer

Journal of medicinal chemistry, 2008-02, Vol.51 (4), p.1068-1072

2008

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Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist

Journal of medicinal chemistry, 2011-07, Vol.54 (13), p.4781-4792

2011

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Knowledge-based chemoinformatic approaches to drug discovery

Drug discovery today, 2006-12, Vol.11 (23), p.1107-1114

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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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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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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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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1,2-Benzothiazine 1,1-dioxide α-ketoamide analogues as potent calpain I inhibitors

Bioorganic & medicinal chemistry letters, 2004-02, Vol.14 (4), p.1035-1038

2004

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Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models

Journal of medicinal chemistry, 2008-09, Vol.51 (18), p.5680-5689

2008

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Novel Peptidyl Phosphorus Derivatives as Inhibitors of Human Calpain I

Journal of medicinal chemistry, 1998-09, Vol.41 (20), p.3912-3916

1998

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Antipicornavirus activity of tetrazole analogs related to disoxaril

Journal of medicinal chemistry, 1993-10, Vol.36 (22), p.3240-3250

1993

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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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A simple synthetic protocol for the protection of amides, lactams, ureas, and carbamates

Tetrahedron letters, 2002-11, Vol.43 (45), p.8063-8066

2002

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Antirhinoviral activity of heterocyclic analogs of Win 54954

Journal of medicinal chemistry, 1992-11, Vol.35 (24), p.4628-4633

1992

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Syntheses of C12,N13 Heterocyclic Bridged Fused Indenopyrrolocarbazoles

Journal of organic chemistry, 2002-05, Vol.67 (10), p.3235-3241

2002

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Overview of Drug Discovery and Development

Current Protocols in Pharmacology, 2006-12, Vol.35 (1), p.9.9.1-9.9.26

2006

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CEP-26401 (Irdabisant), a Potent and Selective Histamine H 3 Receptor Antagonist/Inverse Agonist with Cognition-Enhancing and Wake-Promoting Activities

The Journal of pharmacology and experimental therapeutics, 2012-01, Vol.340 (1), p.124-133

2012

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Calpain inhibitors based on the quiescent affinity label concept: high rates of calpain inactivation with leaving groups derived from N-hydroxy peptide coupling reagents

Bioorganic & medicinal chemistry letters, 2000-10, Vol.10 (20), p.2315-2319

2000

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Synthesis and Biological Activity of a Series of Potent Fluoromethyl Ketone Inhibitors of Recombinant Human Calpain I

Journal of medicinal chemistry, 1997-11, Vol.40 (23), p.3820-3828

1997

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d-Amino Acid Containing, High-Affinity Inhibitors of Recombinant Human Calpain I

Journal of medicinal chemistry, 1998-07, Vol.41 (15), p.2663-2666

1998

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Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles

Journal of medicinal chemistry, 1992-05, Vol.35 (10), p.1663-1670

1992

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Construction of a kinase inhibitor library via parallel synthesis

Tetrahedron letters, 2002-01, Vol.43 (2), p.217-220

2002

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Knowledge Based Prediction of Ligand Binding Modes and Rational Inhibitor Design for Kinase Drug Discovery

Discovery of a Potent, Selective, and Orally Active Proteasome Inhibitor for the Treatment of Cancer

Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist

Knowledge-based chemoinformatic approaches to drug discovery

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

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

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

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

1,2-Benzothiazine 1,1-dioxide α-ketoamide analogues as potent calpain I inhibitors

Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models

Novel Peptidyl Phosphorus Derivatives as Inhibitors of Human Calpain I

Antipicornavirus activity of tetrazole analogs related to disoxaril

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

A simple synthetic protocol for the protection of amides, lactams, ureas, and carbamates

Antirhinoviral activity of heterocyclic analogs of Win 54954

Syntheses of C12,N13 Heterocyclic Bridged Fused Indenopyrrolocarbazoles

Overview of Drug Discovery and Development

CEP-26401 (Irdabisant), a Potent and Selective Histamine H 3 Receptor Antagonist/Inverse Agonist with Cognition-Enhancing and Wake-Promoting Activities

Calpain inhibitors based on the quiescent affinity label concept: high rates of calpain inactivation with leaving groups derived from N-hydroxy peptide coupling reagents

Synthesis and Biological Activity of a Series of Potent Fluoromethyl Ketone Inhibitors of Recombinant Human Calpain I

d-Amino Acid Containing, High-Affinity Inhibitors of Recombinant Human Calpain I

Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles

Construction of a kinase inhibitor library via parallel synthesis

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