PMID
Data
Article Title
Organization
6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives

Hoffmann-La Roche
ULK1 inhibitors and methods using same

Salk Institute
Substituted benzylindazoles for use as Bub1 kinase inhibitors in the treatment of hyperproliferative diseases

Bayer Intellectual Property
EZH2 inhibitors

Mirati Therapeutics
Branched 3-phenylpropionic acid derivatives and their use

Bayer Intellectual Property
Pyrazolo[3,4-d]pyrimidine compound or salt thereof

Taiho Pharmaceutical
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof

Pfizer
N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system

Chronos Therapeutics
Cyclopropanamine compound and use thereof

Takeda Pharmaceutical
Methyl oxazole orexin receptor antagonists

Merck Sharp & Dohme
Heterocyclic compounds useful as pim kinase inhibitors

Incyte
Indole carboxamide compounds

Bristol-Myers Squibb
Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors

Incyte
Compounds and their use as BACE inhibitors

Astrazeneca
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors

Array Biopharm
Assays for screening for or identifying an agent or molecule that can block or inhibit AVB3 integrin from forming a complex with KRAS

University of California
Histone demethylase inhibitors

Celgene Quanticel Research
Liver X receptor (LXR) modulators

Ralexar Therapeutics
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-1-yl) ureas as p38 MAP kinase inhibitors

Respivert
CDK2/4/6 inhibitors

Pfizer
Fused bicyclic compounds for the treatment of disease

Akarna Therapeutics
T-type calcium channel modulator and uses thereof

Uti Limited Partnership
Inhibitors of metallo-beta-lactamase (MBL) comprising a zinc chelating moiety

Universitetet | Oslo
Pyridyl benzothiophenes as kinase inhibitors

Allergan
C-linked heterocycloaklyl substituted pyrimidines and their uses

Genentech
Serine/threonine kinase inhibitors

Genentech
Inhibitor compounds of phosphodiesterase type 10A

Abbvie Deutschland
Aminoquinazoline and pyridopyrimidine derivatives

Genentech
Cycloalkane derivatives

Daiichi Sankyo
Intermediates for preparing triazole agonists of the APJ receptor

Amgen
Compositions and methods for treating ocular diseases

Aerpio Therapeutics
Amlexanox analogs

University of Michigan
Substituted 2-phenyl (AZA)benzofuran compounds for the treatment of hepatitis C

Bristol-Myers Squibb
Xanthine derivatives, their use as a medicament, and pharmaceutical preparations comprising the same

Max-DelbrÜCk-Centrum FÜR Molekulare Medizin
2-heteroaryl carboxamides

Bayer Intellectual Property
Solid dispersions containing an apoptosis-inducing agent

Abbvie
Compounds and methods for inhibiting production of trimethylamine

The Procter & Gamble
Selective glycosidase inhibitors and uses thereof

Alectos Therapeutics
Oxazolidine-based compound and selective androgen receptor agonist comprising same

Dong-A St
Factor XIa inhibitors

Merck Sharp & Dohme
Macrocycles as factor XIa inhibitors

Bristol-Myers Squibb
Pyridineamine compounds useful as Pim kinase inhibitors

Incyte
Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof

The United States of America, As Represented By The Secretary, Department of Health and Human Services
Compounds as diacylglycerol acyltransferase inhibitors

Glaxosmithkline
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors

Array Biopharma
Substituted quinazolines as receptor-type kinase inhibitors

Symphony Evolution
Glucocerebrosidase modulators and uses thereof

Alectos Therapeutics
Aminopyrimidine derivatives for use as modulators of kinase activity

Merck Patent
Phenyl and pyridinyl substituted piperidines and piperazines as inhibitors of IDH1 mutants and their use in treating cancer

Agios Pharmaceuticals
Cyclopropanecarboxylic acid derivative

Daiichi Sankyo
Drug design with a new transition state analog of the hydrated carbonyl: silicon-based inhibitors of the HIV protease.

State University of New York
Energetic, structural, and antimicrobial analyses of beta-lactam side chain recognition by beta-lactamases.

Northwestern University
Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production.

Abbott Laboratories
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.

Merck Research Laboratories
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase.

Berlex Biosciences
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.

Bristol-Myers Squibb
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.

Institut Claudius Regaud
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.

University of Tokyo
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.

Institut De Biologie Structurale
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.

Universite Paris 7-Denis Diderot
Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives.

Peking University
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.

Merck Research Laboratories
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.

Wyeth Research
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.

Wyeth Research
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.

St. Jude Research Hospital
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.

University of Mississippi
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.

Friedrich Alexander University Erlangen
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.

Bristol-Myers Squibb
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species.

Gsk
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.

University Di Perugia
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.

University of North Carolina at Chapel Hill
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.

Universita Degli Studi Di Bari
Structure-activity relationships of C6-uridine derivatives targeting plasmodia orotidine monophosphate decarboxylase.

Toronto General Research Institute
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.

University of Arizona Tucson
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.

Abbott Laboratories
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.

Wyeth Research
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.

University of Arizona Tucson
Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.

Gsk
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.

Gsk
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.

Bristol-Myers Squibb
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.

Karo Bio
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor.

Karo Bio
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.

Karo Bio
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.

Ligand Pharmaceuticals
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.

Gsk
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.

Crefsip
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.

Crefsip
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.

Gsk
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.

University of Tennessee At Knoxville
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.

Daiichi Pharmaceutical
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.

Amgen
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.

Amgen
Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme.

Nci-Fcrdc
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.

Berlex Biosciences
Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.

Abbott Laboratories
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.

Johnson & Johnson Pharmaceutical
Evaluating scoring functions for docking and designing beta-secretase inhibitors.

Merck Research Laboratories
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.

Merck Research Laboratories
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.

Pfizer
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.

Vernalis (R&D)
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.

Abbott Laboratories
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain.

University of Copenhagen
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis.

Suny Stony Brook
Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.

Sunesis
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.

Purdue University
Strong solute-solute dispersive interactions in a protein-ligand complex.

University of Leeds