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352 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.EBI
East China Normal University
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.EBI
Principia Biopharma
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Spiro Meroterpenoids from Ganoderma applanatum.EBI
Chinese Academy Of Sciences
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.EBI
Pfizer
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.EBI
National University Of Singapore
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.EBI
Kasetsart University
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).EBI
Takeda California
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.EBI
Central China Normal University
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing aEBI
Dalian Medical University
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.EBI
University Of Auckland
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.EBI
Merck
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI
Southeast University
Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.EBI
Konkuk 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.EBI
Nerviano Medical Sciences
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.EBI
Shandong University
Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.EBI
China Pharmaceutical University
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes For Biomedical Research
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.EBI
Merck
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.EBI
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).EBI
Icahn School Of Medicine At Mount Sinai
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.EBI
Astrazeneca
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.EBI
Amgen
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI
Kangwon National University
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.EBI
Konkuk University
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI
Sichuan University
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.EBI
Bristol-Myers Squibb R & D
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI
Hanyang University
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.EBI
Bristol-Myers Squibb Research & Development
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.EBI
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.EBI
Xi'An Jiaotong University
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.EBI
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.EBI
Nerviano Medical Sciences
Development of Selective Covalent Janus Kinase 3 Inhibitors.EBI
Harvard Medical School
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI
Astrazeneca
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.EBI
Hoffmann-La Roche
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.EBI
Astellas Pharma
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI
Astellas Pharma
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.EBI
Bristol-Myers Squibb
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.EBI
Pfizer
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
Nerviano Medical Sciences
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.EBI
Syncom
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI
Lexicon Pharmaceuticals
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.EBI
Bristol-Myers Squibb
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI
Galapagos
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.EBI
Pfizer
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.EBI
Peking University
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI
Bristol-Myers Squibb Research And Development
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.EBI
Merck
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.EBI
University Of Toronto
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.EBI
Fox Chase Chemical Diversity Center
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.EBI
Astrazeneca
Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.EBI
Konkuk University
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI
Nerviano Medical Sciences
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.EBI
Genentech
Selectivity data: assessment, predictions, concordance, and implications.EBI
Eli Lilly
Lead identification of novel and selective TYK2 inhibitors.EBI
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 EBI
Genomics Institute Of The Novartis Research Foundation
Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.EBI
Argenta Discovery
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.EBI
Genentech
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.EBI
Genentech
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.EBI
Astrazeneca
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.EBI
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.EBI
F. Hoffmann-La Roche
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.EBI
F. Hoffmann-La Roche
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer
Naphthyl ketones: a new class of Janus kinase 3 inhibitors.EBI
Astrazeneca
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.EBI
Amgen
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI
Glaxosmithkline
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI
Exelixis
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
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 lymphEBI
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.EBI
Sichuan University
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI
Genentech
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.EBI
Genentech
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.EBI
Argenta Discovery
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI
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.EBI
Cephalon
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.EBI
Sichuan University
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 arthEBI
S Bio
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI
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.EBI
Ambit Biosciences
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI
Abbott Laboratories
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.EBI
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.EBI
Astrazeneca R&D
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.EBI
Sri International
Features of selective kinase inhibitors.EBI
University Of California San Francisco
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.EBI
Vertex Pharmaceuticals
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.EBI
Amgen
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.EBI
Vertex Pharmaceuticals
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.EBI
Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI
Bristol-Myers Squibb Research And Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI
Amgen
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.EBI
Amgen
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.EBI
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.EBI
Abbott Laboratories
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).EBI
Procter And Gamble Pharmaceuticals
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.EBI
Procter And Gamble Pharmaceuticals
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI
Astrazeneca
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.EBI
University Of Kentucky
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI
Ludwig-Maximilians University Of Munich
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.EBI
Amgen
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.EBI
Cephalon
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Ansaris
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.EBI
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.EBI
Novartis Institute For Biomedical Research
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI
Bristol-Myers Squibb
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI
Ariad Pharmaceuticals
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.EBI
Astrazeneca R&D Boston
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI
Nerviano Medical Sciences
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI
Vertex Pharmaceuticals
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI
TBA
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.EBI
Bristol-Myers Squibb
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI
TBA
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.EBI
Pfizer
5-amino-pyrazoles as potent and selective p38a inhibitors.EBI
Bristol-Myers Squibb Research And Development
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI
Nerviano Medical Sciences Oncology
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.EBI
Université
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI
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.EBI
Abbott Laboratories
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.EBI
Novartis Institutes For Biomedical Research
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.EBI
Novartis Institutes For Biomedical Research
2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.EBI
Ligand Pharmaceuticals
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).EBI
Cytopia Research
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.EBI
Astrazeneca R&D Boston
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.EBI
Vertex Pharmaceuticals
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
Vertex Pharmaceuticals
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.EBI
Johnson & Johnson Pharmaceutical Research & Development
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
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).EBI
National Human Genome Research Institute
Fragment-based discovery of JAK-2 inhibitors.EBI
Sgx Pharmaceuticals
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.EBI
Amgen
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI
Amgen
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.EBI
The Scripps Research Institute
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.EBI
Amgen
Simplified staurosporine analogs as potent JAK3 inhibitors.EBI
Johnson & Johnson Pharmaceutical Research And Development
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI
Amgen
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.EBI
Pharmaceutical Research Institute
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI
Abbott Bioresearch Center
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI
Bristol-Myers Squibb
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Mapping the kinase domain of Janus Kinase 3.EBI
Aventis Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.EBI
Aventis Pharmaceuticals
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI
Merck Research Laboratories
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI
Merck Research Laboratories
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.EBI
Japan Tobacco
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.EBI
East China University Of Science & Technology
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.EBI
University Of Strathclyde
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.EBI
Takeda Pharmaceutical
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.EBI
Shenyang Pharmaceutical University
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.EBI
Pfizer
Identification of EBI
China Pharmaceutical University
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.EBI
Dalian Medical University
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.EBI
Gvk Biosciences
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.EBI
Chia Tai Tianqing Pharmaceutical Group
Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI
Peking University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.EBI
China Pharmaceutical University
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.EBI
Glaxosmithkline R&D
Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors.EBI
Leo Pharma
Small-molecule agents for the treatment of inflammatory bowel disease.EBI
Gilead Sciences
Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1EBI
Shandong University
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.EBI
Gwangju Institute Of Science And Technology (Gist)
Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3.EBI
Astellas Pharma
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.EBI
TBA
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI
TBA
Identification of EBI
TBA
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).EBI
Pfizer
Discovery of (2EBI
Astrazeneca
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.EBI
Janssen Research And Development
Identification of Imidazo[1,2-EBI
Bristol-Myers Squibb
Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.EBI
China Pharmaceutical University
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.EBI
Vertex Pharmaceuticals
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.EBI
Glaxosmithkline R&D
Discovery of 4EBI
TBA
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.EBI
TBA
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI
TBA
The Exploration of Chirality for Improved Druggability within the Human Kinome.EBI
University Of Arkansas For Medical Sciences
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.EBI
Eberhard Karls University T£Bingen
Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).EBI
Peking University
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.EBI
Shandong University
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.EBI
Sichuan University And Collaborative Innovation Center
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.EBI
Arromax Pharmatech
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.EBI
East China University Of Science & Technology
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.EBI
Central China Normal University
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.EBI
Southeast University
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.EBI
Bristol-Myers Squibb
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.EBI
Peking University
Targeting the immunity protein kinases for immuno-oncology.EBI
China Pharmaceutical University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
University Of Florida
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.EBI
West China Hospital Of Sichuan University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Overview of Recent Strategic Advances in Medicinal Chemistry.EBI
Shandong University
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.EBI
Genentech
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.EBI
Pfizer
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI
Novartis Institutes For Biomedical Research
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI
Universitaire Vaudois
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.EBI
National University Of Singapore
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.EBI
Pfizer
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.EBI
Purdue University
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.EBI
Yunnan University
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.EBI
Beijing Normal University
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.EBI
The First Affiliated Hospital Of Dalian Medical University
Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.EBI
Astellas Pharma
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.EBI
China Pharmaceutical University
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.EBI
Bristol-Myers Squibb
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.EBI
Dalian Medical University
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives.EBI
Universit£
Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.EBI
Seoul National University
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.EBI
Eberhard-Karls-University Tuebingen
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.EBI
Advinus Therapeutics
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.EBI
Shaanxi University Of Science & Technology
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.EBI
Second Military Medical University
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.EBI
Astrazeneca
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.EBI
University Of Science And Technology Of China
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.EBI
Eberhard Karls University T£Bingen
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.EBI
Sichuan University And Collaborative Innovation Center
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.EBI
Bristol-Myers Squibb Research And Development
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI
The Ohio State University
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.EBI
Bristol-Myers Squibb
Discovery of highly potent, selective, covalent inhibitors of JAK3.EBI
Bristol-Myers Squibb Research And Development
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.EBI
Genentech
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.EBI
Merck
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.EBI
National University Of Singapore
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.EBI
University Of Science And Technology Of China
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.EBI
Pfizer
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.EBI
Therachem Research Medilab (India)
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.EBI
Moffitt Cancer Center
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.EBI
Wuxi Apptec (Shanghai)
A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.BDB
A*Star
Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.BDB
Nas Of Ukraine
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.BDB
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.BDB
Case Western Reserve University School Of Medicine
Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.BDB
Griffith University
Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.BDB
Panjab University
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.BDB
Takeda Chemical Industries
Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.BDB
Creighton University
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.BDB
University Of Colorado
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.BDB
F. Hoffmann-La Roche
Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.BDB
New York University
High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.BDB
Nankai University
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.BDB
National Institute Of Mental Health
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.BDB
Duke University Medical Center
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.BDB
Cyclacel
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.BDB
Yale University
Identification of a potent new chemotype for the selective inhibition of PDE4.BDB
Nih
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.BDB
Universita Del Piemonte Orientale
Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.BDB
Gilead Sciences
Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids.BDB
The Johns Hopkins University
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.BDB
Gsk
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.BDB
Astrazeneca
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.BDB
Lund University
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.BDB
Morphochem
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.BDB
Johns Hopkins University
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).BDB
University Of Illinois At Chicago
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.BDB
Axys Pharmaceutical
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.BDB
Glaxosmithkline
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.BDB
Glaxosmithkline
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).BDB
Istituto Di Cristallografia
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.BDB
University Of Bologna
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.BDB
Wyeth-Ayerst Research
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.BDB
Merck Research Laboratories