55 articles for thisTarget
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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
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
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
Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
Novartis
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
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 pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators
Janssen Pharmaceutica
Substituted tetrahydrocarbazole and carbazole carboxamide compounds
Bristol-Myers Squibb
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
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