PMID

Data

Article Title

Organization

Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.

Millennium Pharmaceuticals

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.

Millennium Pharmaceuticals

Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors.

Millennium Pharmaceuticals

Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.

Millennium Pharmaceuticals

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals

Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).

Millennium Pharmaceuticals

Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.

Millennium Pharmaceuticals

Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Millennium Pharmaceuticals

Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.

Millennium Pharmaceuticals

Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.

Millennium Pharmaceuticals

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.

Millennium Pharmaceuticals

Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.

Millennium Pharmaceuticals

A new dimeric dihydrochalcone and a new prenylated flavone from the bud covers of Artocarpus altilis: potent inhibitors of cathepsin K.

Millennium Pharmaceuticals

Small molecule antagonists of the CC chemokine receptor 4 (CCR4).

Millennium Pharmaceuticals

Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.

Millennium Pharmaceuticals

Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4.

Millennium Pharmaceuticals

Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).

Millennium Pharmaceuticals

Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.

Millennium Pharmaceuticals

Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists.

Millennium Pharmaceuticals

Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).

Millennium Pharmaceuticals

N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.

Millennium Pharmaceuticals

Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.

Millennium Pharmaceuticals

Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.

Millennium Pharmaceuticals

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.

Millennium Pharmaceuticals

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.

Millennium Pharmaceuticals

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

Millennium Pharmaceuticals

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.

Millennium Pharmaceuticals

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

Metal coordination-based inhibitors of adenylyl cyclase: novel potent P-site antagonists.

Millennium Pharmaceuticals

Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.

Millennium Pharmaceuticals

Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.

Millennium Pharmaceuticals

Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.

Millennium Pharmaceuticals

Design and synthesis of factor Xa inhibitors and their prodrugs.

Millennium Pharmaceuticals

Hydroxamate based inhibitors of adenylyl cyclase. Part 2: the effect of cyclic linkers on P-site binding.

Millennium Pharmaceuticals

Hydroxamate based inhibitors of adenylyl cyclase. Part 1: the effect of acyclic linkers on P-site binding.

Millennium Pharmaceuticals

Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.

Millennium Pharmaceuticals

Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.

Millennium Pharmaceuticals

Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.

Millennium Pharmaceuticals

Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.

Millennium Pharmaceuticals

BTK inhibitor compounds

Eli Lilly

Biaryl urea derivative or salt thereof and preparation process and use for the same

Fudan University

Composition and methods for inhibiting mammalian sterile 20-like kinase 1

The Scripps Research Institute

3-azabicyclo[3.1.0]hexane derivative and use thereof for medical purpose

Sanwa Kagaku Kenkyusho

Pyrrolidinyl sulfone RORγ modulators

Bristol-Myers Squibb

8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions

Boehringer Ingelheim International

Synthesis of readily available fluorophenylalanine derivatives and investigation of their biological activity.

Charles University

Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As ß-glucuronidase inhibitors.

Universiti Teknologi Mara (Uitm)

Piperidylpyrimidine derivatives as modulators of protein kinase inhibitors and of vascular endothelial growth factor receptor 2

Allergan

Compounds for the treatment of neurodegenerative diseases

Katholieke Universiteit Levun

Inhibitors of human EZH2, and methods of use thereof

Epizyme

Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.

Technical University of Munich

Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.

Glaxosmithkline