PMID

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Article Title

Organization

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai

Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.

Sichuan University

Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.

Bristol-Myers Squibb Research and Development

Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.

Califia Bio

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.

Glaxosmithkline

1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.

Glaxosmithkline

4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.

Glaxosmithkline

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.

Glaxosmithkline

Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.

Korea University

Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of I¿B kinase-ß.

Universidade Federal Do Rio De Janeiro

The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.

Boehringer Ingelheim Pharmaceuticals

Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.

Glaxosmithkline

Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors.

Ucb Pharma

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.

Kyoto 619-0216

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Bristol-Myers Squibb Research and Development

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.

Pfizer

Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.

Korea Institute of Science and Technology

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Vertex Pharmaceuticals

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.

Glaxosmithkline

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.

TBA

Novel dihydrothieno[2,3-e]indazole derivatives as I&x3ba;B kinase inhibitors.

Kyorin Pharmaceutical

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Bristol-Myers Squibb

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.

Daiichi Sankyo

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

Wyeth Research

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Wyeth Research

Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wyeth Research

Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.

Pfizer

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Nerviano Medical Sciences

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Bristol-Myers Squibb Research and Development

Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Wyeth Research

From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.

University of Illinois At Chicago

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

Wyeth Research

Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.

Boehringer Ingelheim Pharmaceuticals

Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.

Novartis Institutes For Biomedical Research

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.

Kyoto 619-0216

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.

Kyoto 619-0216

Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy.

Alexandria University

A novel series of potent and selective IKK2 inhibitors.

Celltech R&D

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

Quinolone hybrids and their anti-cancer activities: An overview.

Qilu University of Technology (Shandong Academy of Sciences)

Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Merck

Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.

Glaxosmithkline R&D

Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.

Glaxosmithkline R&D

Discovery of 4

TBA

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.

Glaxosmithkline

Inhibitory Kappa B Kinaseα (IKKα) Inhibitors That Recapitulate Their Selectivity in Cells against Isoform-Related Biomarkers.

University of Strathclyde

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

Merck Sharp & Dohme

Substituted 6,5-fused bicyclic heteroaryl compounds

Epizyme

Oxazolidinone and imidazolidinone compounds

Hoffmann-La Roche

1,2,3-triazole-4-amine derivatives for the treatment of sigma receptor related diseases and disorders

Laboratorios Del Dr. Esteve

Phenyloxadiazole derivatives as PGDS inhibitors

Sanofi

Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.

Ondokuz Mayis University

a-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters.

Dumlupinar University

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

Merck Research Laboratories

Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes.

Universita Degli Studi