PMID

Data

Article Title

Organization

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

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

Pharmacological properties of recombinant "diazepam-insensitive" GABAA receptors.

National Institute Of Diabetes, Digestive And Kidney Diseases

Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.

The Scripps Research Institute

Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.

University Of Pennsylvania

Cloning and expression of a human somatostatin-14-selective receptor variant (somatostatin receptor 4) located on chromosome 20.

University Of Toronto

Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics.

Mayo Foundation

Selective alpha-2 adrenoceptor blockade by SK&F 86466: in vitro characterization of receptor selectivity.

Smith Kline & French Laboratories

Characterization of the binding of [3H]-CGS 19755: a novel N-methyl-D-aspartate antagonist with nanomolar affinity in rat brain.

Ciba-Geigy

Highly potent and selective ligands for a new class H3 of histamine receptor.

UnitÉ