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351 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27983835 81 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
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck
27490956 59 Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.EBI Merck
27288183 130 Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI Southeast University
27261178 32 Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.EBI Konkuk University
27003761 120 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
27137359 18 Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.EBI Shandong University
27117263 51 Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.EBI Takeda Pharmaceutical
26951750 59 Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes For Biomedical Research
26819674 66 Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.EBI Genentech
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes For Biomedical Research
26927423 58 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.EBI Merck
26701356 100 Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.EBI Takeda Pharmaceutical
26762835 342 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
26614408 106 Identification of azabenzimidazoles as potent JAK1 selective inhibitors.EBI Astrazeneca
26396685 19 Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.EBI Amgen
26351728 96 Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.EBI Konkuk University
26288683 43 Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.EBI Bristol-Myers Squibb R & D
26288682 64 Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.EBI Bristol-Myers Squibb Research & Development
26086931 38 Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.EBI Shandong University
26222319 192 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
26258521 104 Development of Selective Covalent Janus Kinase 3 Inhibitors.EBI Harvard Medical School
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI Astrazeneca
25262541 86 Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.EBI Hoffmann-La Roche
26059596 58 Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.EBI Astellas Pharma
26071372 89 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
25987372 104 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.EBI Bristol-Myers Squibb
25353650 111 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
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24930833 136 Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.EBI Syncom
25453808 101 Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.EBI Bristol-Myers Squibb
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos
24417533 63 Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.EBI Pfizer
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24461299 82 Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.EBI Fox Chase Chemical Diversity Center
24359159 60 Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.EBI Astrazeneca
24398382 3 Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.EBI Konkuk University
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences
24042009 89 Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.EBI Genentech
23867602 122 Lead identification of novel and selective TYK2 inhibitors.EBI Genentech
23742252 81 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
23642482 62 Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.EBI Argenta Discovery
23668484 15 Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.EBI Genentech
23659214 138 Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.EBI Genentech
23541670 63 Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.EBI Hoffmann-La Roche
23540648 103 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
23265875 78 Design and synthesis of tricyclic cores for kinase inhibition.EBI Abbott Bioresearch Center
23214979 74 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
10741557 26 Naphthyl ketones: a new class of Janus kinase 3 inhibitors.EBI Astrazeneca
21903390 79 Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI Glaxosmithkline
23127890 96 SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI Exelixis
23107482 82 Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.EBI Genentech
22726925 216 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.EBI Cellzome
21604762 152 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
23116168 42 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
23061660 92 Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI Genentech
22698084 99 Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.EBI Genentech
22591402 127 Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.EBI Argenta Discovery
22594690 80 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
22339472 148 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
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen
22168626 32 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
21155605 39 Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.EBI Novartis Institutes For Biomedical Research
21106455 60 Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.EBI Sri International
19648005 41 Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.EBI Amgen
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
22136433 67 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
22087750 145 Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.EBI Amgen
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21942426 113 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
21936542 143 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
21561767 48 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI Ariad Pharmaceuticals
21470862 110 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
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21105711 79 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
21038853 133 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI Novartis Institutes For Biomedical Research
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20231096 81 Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.EBI Novartis Institutes For Biomedical Research
20138510 60 2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.EBI Novartis Institutes For Biomedical Research
19762238 78 Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).EBI Cytopia Research
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences
19053756 27 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
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
12482439 51 Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI Merck Research Laboratories
32511913 141 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
32122740 27 Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.EBI East China University of Science & Technology
32001089 8 Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.EBI University of Strathclyde
31980341 31 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
32527540 51 Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.EBI Shenyang Pharmaceutical University
32253095 78 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
32479083 42 Identification of EBI China Pharmaceutical University
32462873 216 Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.EBI Gvk Biosciences
31843459 57 Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.EBI Chia Tai Tianqing Pharmaceutical Group
31831383 2 Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34.EBI Brigham Young University
31757666 314 Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI Merck
30853331 95 Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.EBI China Pharmaceutical University
30833158 51 The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors.EBI Hungarian Academy of Sciences
27491711 422 Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI Merck And
27326341 142 Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors.EBI Leo Pharma
27578246 158 Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.EBI Glaxosmithkline R&D
27774135 6 Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1EBI Shandong University
27555284 27 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)
27544589 52 Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3.EBI Astellas Pharma
31609613 244 Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.EBI TBA
31314518 356 Identification of EBI TBA
30113844 240 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
32297743 59 Discovery of (2EBI Astrazeneca
32134643 66 Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.EBI Janssen Research and Development
30891145 70 Identification of Imidazo[1,2-EBI Bristol-Myers Squibb
30846405 102 Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.EBI China Pharmaceutical University
31693351 473 Discovery of 4EBI TBA
31318208 123 Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.EBI TBA
31550151 17 The Exploration of Chirality for Improved Druggability within the Human Kinome.EBI University of Arkansas For Medical Sciences
30565923 34 Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.EBI Eberhard Karls University T£Bingen
30901208 96 Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.EBI Shandong University
30878832 57 Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.EBI Arromax Pharmatech
30981578 46 Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.EBI East China University of Science & Technology
30926315 75 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
30987781 88 Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.EBI Southeast University
30891131 60 Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.EBI Bristol-Myers Squibb
31647655 114 Kinase Chemodiversity from the Arctic: The Breitfussins.EBI Uit - The Arctic University of Norway
30530193 64 Targeting the immunity protein kinases for immuno-oncology.EBI China Pharmaceutical University
30384048 365 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
31670517 41 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
31050421 48 Overview of Recent Strategic Advances in Medicinal Chemistry.EBI Shandong University
29870256 16 Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.EBI Genentech
28139931 85 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
26505898 123 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
31200237 95 Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI Shanghai Pharmaceuticals Holding
29969256 21 Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI Universitaire Vaudois
30243158 80 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
30170943 35 Design and synthesis of potent RSK inhibitors.EBI Novartis Institutes For Biomedical Research
30423248 226 Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.EBI Pfizer
30460842 111 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
30145050 27 Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.EBI Astellas Pharma
30139575 98 Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.EBI China Pharmaceutical University
29452839 82 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
28844493 14 Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.EBI Eberhard-Karls-University Tuebingen
28279528 53 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
29631132 33 The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.EBI Shaanxi University of Science & Technology
29940115 55 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
29856615 85 Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.EBI Astrazeneca
29852068 86 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
28734581 37 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
28539220 198 Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.EBI Bristol-Myers Squibb Research and Development
28927786 52 Discovery of highly potent, selective, covalent inhibitors of JAK3.EBI Bristol-Myers Squibb Research and Development
28830649 101 Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.EBI Genentech
29156136 160 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
28953386 66 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
29298069 206 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
28626521 4 Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.EBI Yale University
28626517 24 Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.EBI Therachem Research Medilab (India)
34271072 34 A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.BDB A*Star
23578312 22 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
22233543 70 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
28181373 14 Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.BDB Griffith University
28126289 11 Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.BDB Panjab University
22339993 8 Inhibition of bacterial virulence: drug-like molecules targeting the Salmonella enterica PhoP response regulator.BDB Washington University
11909603 1 T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.BDB Takeda Chemical Industries
11164381 20 Stereochemistry and molecular pharmacology of (S)-thio-ATPA, a new potent and selective GluR5 agonist.BDB The Royal Danish School of Pharmacy
10604951 12 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
9103528 17 PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.BDB Pharmacia & Upjohn
12210991 24 Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.BDB New York University
6310078 55 Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, a new uptake inhibitor with selectivity for serotonin.BDB Pfizer
19101476 5 The importance of odorant conformation to the binding and activation of a representative olfactory receptor.BDB Columbia University
16492568 12 Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.BDB Cyclacel
17433696 19 Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.BDB Astrazeneca
19692239 23 Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.BDB Boehringer Ingelheim Pharmaceuticals
19179081 32 Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.BDB Yale University
18243697 77 Identification of a potent new chemotype for the selective inhibition of PDE4.BDB Nih
19464171 87 Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.BDB Amgen
19361197 54 Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.BDB Universita Del Piemonte Orientale
18954041 28 Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).BDB University of Michigan
18811140 11 Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.BDB Merck Research Laboratories
18714982 44 Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.BDB Cephalon
18341273 16 Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.BDB Astrazeneca
16242339 63 Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.BDB Lund University
14521405 29 Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.BDB Bristol-Myers Squibb
10903938 20 Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.BDB Novartis Pharmaceuticals
12946343 3 The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.BDB Morphochem
17114291 10 Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.BDB Johns Hopkins University
11520194 13 Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).BDB University of Illinois At Chicago
11731301 192 Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.BDB Axys Pharmaceutical
17201404 16 Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.BDB Glaxosmithkline
12061878 100 Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.BDB Aventis Pharma Deutschland
16434195 23 Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
16982190 46 Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.BDB Glaxosmithkline
16913695 12 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
16919457 144 Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.BDB Merck Research Laboratories
12773032 4 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
16616489 29 Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.BDB Institut Curie
14552750 35 Identification of potent and novel small-molecule inhibitors of caspase-3.BDB Sunesis Pharmaceuticals
15012993 22 A new series of potent oxindole inhibitors of CDK2.BDB Hoffmann-La Roche
12699760 19 5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB Glaxosmithkline
15916442 52 Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.BDB Wyeth Research
11728184 20 Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.BDB Biocryst Pharmaceuticals
11689083 41 Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.BDB Wyeth-Ayerst Research
7520079 13 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
9171880 21 Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors.BDB Dupont Pharmaceuticals