PMID

Data

Article Title

Organization

Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.

Southeast University

Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.

Konkuk University

Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.

Zhejiang University

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.

Nerviano Medical Sciences

Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.

Shandong University

Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.

China Pharmaceutical University

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Genentech

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.

Merck

Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.

Takeda Pharmaceutical

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

Identification of azabenzimidazoles as potent JAK1 selective inhibitors.

Astrazeneca

Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.

Kangwon National University

Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.

Konkuk University

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Bristol-Myers Squibb R & D

Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

Bristol-Myers Squibb Research & Development

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.

Shandong University

Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.

Xi'An Jiaotong University

Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.

China Pharmaceutical University

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

Nerviano Medical Sciences

Development of Selective Covalent Janus Kinase 3 Inhibitors.

Harvard Medical School

Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.

Zhejiang University

Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.

Astrazeneca

Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.

Hoffmann-La Roche

Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.

Astellas Pharma

Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.

Astellas Pharma

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Bristol-Myers Squibb

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.

Vertex Pharmaceuticals

(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.

Genomics Institute Of The Novartis Research Foundation

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

Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.

University Of South Florida

Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.

Central South University

Discovery and profiling of a selective and efficacious Syk inhibitor.

Novartis Institutes For Biomedical Research

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.

Nerviano Medical Sciences

Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.

Vertex Pharmaceuticals

Computer-aided discovery of aminopyridines as novel JAK2 inhibitors.

Chonnam National University

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

Pfizer

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.

Nerviano Medical Sciences

Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.

Syncom

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.

Merck Research Laboratories

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.

Lexicon Pharmaceuticals

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Bristol-Myers Squibb

A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.

Zhejiang University

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.

Genentech

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Galapagos

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Merck Research Laboratories

2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.

Novartis Institutes For Biomedical Research

Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.

Pfizer

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Nerviano Medical Sciences

Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.

Gilead Sciences

Syk inhibitors with high potency in presence of blood.

Novartis Institutes For Biomedical Research

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

Bristol-Myers Squibb Research And Development

Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.

Merck

The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.

Merck

Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.

University Of Zurich

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Pfizer

A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.

University Of Toronto

Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.

Fox Chase Chemical Diversity Center

Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.

Zhejiang University

Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Astrazeneca

Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.

University Of Zurich

Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.

Konkuk University

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).

Nerviano Medical Sciences

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Genentech

Lead identification of novel and selective TYK2 inhibitors.

Genentech

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

Genentech

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase

Genomics Institute Of The Novartis Research Foundation

Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.

Argenta Discovery

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Genentech

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Genentech

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

Merck Research Laboratories

Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.

Merck Research Laboratories

Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.

Astrazeneca

Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.

Merck Research Laboratories

Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.

Hoffmann-La Roche

Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.

F. Hoffmann-La Roche

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

Exelixis

Design and synthesis of tricyclic cores for kinase inhibition.

Abbott Bioresearch Center

3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.

F. Hoffmann-La Roche

Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.

Glaxosmithkline

SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.

Exelixis

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph

S*Bio

Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.

Sichuan University

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Genentech

Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

Genentech

Discovery and development of spleen tyrosine kinase (SYK) inhibitors.

Rigel

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Genentech

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

Exelixis

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

TBA

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.

Argenta Discovery

Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.

Janssen Pharmaceutical Companies Of Johnson & Johnson

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Abbott Laboratories

A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.

Cephalon

Structure-based optimization of aminopyridines as PKC¿ inhibitors.

Vertex Pharmaceuticals

The design, synthesis, and biological evaluation of PIM kinase inhibitors.

Exelixis

Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.

Hanmi Research Center

Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth

S Bio

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

Amgen

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Ambit Biosciences

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Abbott Laboratories

Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.

TBA

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.

Astrazeneca R&D Boston

Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Merck Research Laboratories

Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.

Novartis Institutes For Biomedical Research

Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.

Astrazeneca R&D

Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.

Merck Research Laboratories

Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

Sri International

3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.

Vertex Pharmaceuticals

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Nerviano Medical Sciences

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.

Vertex Pharmaceuticals

Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.

Amgen

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.

National Cancer Institute-Bethesda

Discovery and development of aurora kinase inhibitors as anticancer agents.

Vertex Pharmaceuticals

Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.

Pfizer

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

University Of Oxford

Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.

Merck Frosst Centre For Therapeutic Research

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

Abbott Laboratories

Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).

Procter And Gamble Pharmaceuticals

Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.

Procter And Gamble Pharmaceuticals

Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Glaxosmithkline

Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase

S Bio

7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.

Ludwig-Maximilians University Of Munich

Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.

Amgen

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.

Cephalon

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Structure-based design of PDK1 inhibitors.

S Bio

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.

Cephalon

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.

Vertex Pharmaceuticals

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.

Merck

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research

Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Merck Research Laboratories

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals

In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.

Astrazeneca R&D Boston

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

Vertex Pharmaceuticals

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

TBA

Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.

Abbott Laboratories

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

Bristol-Myers Squibb

Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.

Abbott Laboratories

Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277

TBA

Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.

Pfizer

The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.

Merck

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Merck Research Laboratories

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Nerviano Medical Sciences Oncology

Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.

Amgen

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

Ambit Biosciences

Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.

Université

New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.

Novartis Institute Of Biomedical Research

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Abbott Laboratories

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Novartis Institutes For Biomedical Research

Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.

Novartis Institutes For Biomedical Research

Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.

Astrazeneca R&D Boston

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Novartis Institutes For Biomedical Research

2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.

Ligand Pharmaceuticals

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

Cytopia Research

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.

Vertex Pharmaceuticals

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

Abbott Laboratories

Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.

Astrazeneca R&D Boston

Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.

Vertex Pharmaceuticals

Design and synthesis of a novel tyrosine kinase inhibitor template.

St. Jude Children'S Research Hospital

Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening.

Semmelweis University

Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.

Vertex Pharmaceuticals

Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.

Astrazeneca R&D Boston

Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).

National Human Genome Research Institute

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

Glaxosmithkline

Fragment-based discovery of JAK-2 inhibitors.

Sgx Pharmaceuticals

Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.

Astrazeneca Pharmaceuticals

Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.

Amgen

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

Genomics Institute Of The Novartis Research Foundation

Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.

University Of Oklahoma Health Sciences Center

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Novartis Institutes For Biomedical Research

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.

Amgen

Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.

Amgen

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.

Aventis Pharmaceuticals

Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.

Merck Research Laboratories

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Merck Research Laboratories

Inhibition of acetylpolyamine and spermine oxidases by the polyamine analogue chlorhexidine.

University Roma Tre

New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.

Centre De Recherche De Gif

Fatty acid-binding protein 5 (FABP5) regulates cognitive function both by decreasing anandamide levels and by activating the nuclear receptor peroxisome proliferator-activated receptor ß/d (PPARß/d) in the brain.

Case Western Reserve University School Of Medicine

Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.

Griffith University

Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.

Panjab University

Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation.

Mcgill University

Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.

Aimst University

Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A.

University Of Kentucky

Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.

I.G.B.M.C.