PMID

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Article Title

Organization

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).

Gsk

Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.

Gsk

The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.

Gsk

Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.

Gsk

Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.

Gsk

Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT).

Gsk

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.

Gsk

Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.

Gsk

Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.

Gsk

Substituted 1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2-a:1',2'-d]pyrazines and methods for treating viral infections

Gilead Sciences

Inhibiting agents for Bruton's tyrosine kinase

Biogen Ma

Factor IXa inhibitors

Merck Sharp & Dohme

Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases

Universite De Lille 2 Droit Et Sante

2-aryl- and 2-arylalkyl-benzimidazoles as mIDH1 inhibitors

Bayer Pharma Aktiengesellschaft

Dihydropyrazolopyrimidinone compounds as PDE2 inhibitors

Merck Sharp & Dohme

Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Array Biopharma

Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors

Array Biopharma

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

Ifm Due

5H-pyrido[3,2-B]indole compounds as anticancer agents

Bristol-Myers Squibb

Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors

Pfizer

Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease

Novartis

Amino-pyrimidine-containing spleen tyrosine kinase (Syk) inhibitors

Merck Sharp & Dohme

Substituted 6,5-fused bicyclic heteroaryl compounds

Epizyme

N-substituted pyrazolo [3,4-D] pyrimidine ketone compound, and preparation process and use thereof

Sun Yat-Sen University

Rho kinase inhibitors and methods of use

H. Lee Moffitt Cancer Center and Research Institute

Substituted piperidine compounds and their use as orexin receptor modulators

Janssen Pharmaceutica

1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors

Angelini Acraf

[8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones

Bayer Pharma Aktiengesellschaft

Compounds and uses

Astrazeneca

Inhibitors of Bruton's tyrosine kinase

Pharmacyclics

Bicyclo[3.2.1]octyl amide derivatives and uses of same

H. Lundbeck

Inhibitors of IRAK4 activity

Merck Sharp & Dohme

Piperidine substituted tricyclic pyrazolo[1,5-a]pyrimidine derivatives with inhibitory activity on the replication of the respiratory syncytial virus (RSV)

Janssen Ireland

Bicyclic heteroaryl derivatives as CFTR potentiators

Cystic Fibrosis Foundation Therapeutics

Substituted tricyclic compounds as FGFR inhibitors

Incyte

Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Array Biopharma

Tied-back benzamide derivatives as potent rock inhibitors

Bristol-Myers Squibb

Benzoxazepin oxazolidinone compounds and methods of use

Genentech

Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators

Janssen Pharmaceutica

Substituted tetrahydrocarbazole and carbazole carboxamide compounds

Bristol-Myers Squibb

INHIBITORS OF TYROSINE KINASE 2 MEDIATED SIGNALING

Abbvie

Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.

Istituto Di Biostrutture E Bioimmagini-Cnr

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight.

University of Padova

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

Johnson & Johnson Pharmaceutical

Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.

National Institutes of Health

Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.

Institut Curie

Nicotinyl aspartyl ketones as inhibitors of caspase-3.

Merck Frosst Canada

Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3.

Glaxosmithkline

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.

Cyclacel

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

Johnson & Johnson Pharmaceutical

Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design.

Banyu Tsukuba Research Institute

Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase.

University of Regensburg