419 articles for thisTarget
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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.
Pfizer
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.
Merck
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
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
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
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
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.
Amgen
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
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
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 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 pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Bristol-Myers Squibb
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Galapagos
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
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.
Fox Chase Chemical Diversity Center
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
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
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
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
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
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Genentech
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 and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Genentech
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Argenta Discovery
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
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
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
Novartis Institutes For Biomedical Research
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
Sri International
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.
Amgen
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
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
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 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Nerviano Medical Sciences
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.
Pfizer
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Novartis Institute of Biomedical Research
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Novartis Institutes For Biomedical Research
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Novartis Institutes For Biomedical Research
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
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
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.
Wuyi University
Sokotrasterol Sulfate Suppresses IFN-γ-Induced PD-L1 Expression by Inhibiting JAK Activity.
Fudan University
Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
China Pharmaceutical University
Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors.
China Pharmaceutical University
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.
University of Arkansas
Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.
Ewha Womans University
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Novartis Institutes For Biomedical Research
Targeting the Tyrosine Kinase 2 (TYK2) Pseudokinase Domain: Discovery of the Selective TYK2 Inhibitor ABBV-712.
Abbvie
Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Shandong University
Clinically approved small-molecule drugs for the treatment of rheumatoid arthritis.
Jilin University
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.
Astrazeneca
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bristol-Myers Squibb
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.
Insilico Medicine Hong Kong
Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer.
Kafrelsheikh University
Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes.
Merck Healthcare
Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.
China Pharmaceutical University
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1.
University of South China
Eyes on Topical Ocular Disposition: The Considered Design of a Lead Janus Kinase (JAK) Inhibitor That Utilizes a Unique Azetidin-3-Amino Bridging Scaffold to Attenuate Off-Target Kinase Activity, While Driving Potency and Aqueous Solubility.
Alcon Research
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
Discovery of novel dual Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) inhibitors as a promising strategy for rheumatoid arthritis.
China Pharmaceutical University
Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
Nimbus Therapeutics
Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Novartis
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
Novartis Institutes For Biomedical Research
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
Biocon-Bristol Myers Squibb Research and Development Center
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.
China Pharmaceutical University
Discovery of tricyclic dipyrrolopyridine derivatives as novel JAK inhibitors.
Astellas Pharma
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.
Universite de Tours
Cyclic tailor-made amino acids in the design of modern pharmaceuticals.
Nanjing Forestry University
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis.
East China Normal University
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Bristol Myers Squibb
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.
Zhuhai United Laboratories
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Tianjin University
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.
Zunyi Medical University
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
China Pharmaceutical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University of Technology
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor.
Cadila Healthcare
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.
Chinese Academy of Sciences
Synthesis and structure-activity relationship studies of 1,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 1 (JAK1) inhibitors.
Gwangju Institute of Science and Technology (Gist)
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
Csir-Indian Institute of Integrative Medicine
Boron-Containing Pyrazole Compounds as JAK Inhibitors for Treating Inflammation, Autoimmune Diseases, and Cancer.
Smith, Gambrell & Russell
Optimization of Pyrimidine Compounds as Potent JAK1 Inhibitors and the Discovery of R507 as a Clinical Candidate.
Rigel Pharmaceuticals
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr
East China Normal University
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Synthesis and evaluation of hydrazinyl-containing pyrrolo[2,3-d]pyrimidine series as potent, selective and oral JAK1 inhibitors for the treatment of rheumatoid arthritis.
Wuxi Apptec (Shanghai) Co.
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.
East China Normal University
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Gsk
Identification of a Novel 2,8-Diazaspiro[4.5]decan-1-one Derivative as a Potent and Selective Dual TYK2/JAK1 Inhibitor for the Treatment of Inflammatory Bowel Disease.
Sichuan University and Collaborative Innovation Center of Biotherapy
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Bristol Myers Squibb
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.
University of Chinese Academy of Science
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
China Pharmaceutical University
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Bristol-Myers Squibb Research & Development
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.
Jinan University
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Merck Research Laboratories
-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
West China Hospital of Sichuan University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
Sichuan University and Collaborative Innovation Center
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Genomics Institute of The Novartis Research Foundation
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Roche Innovation Center Shanghai
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Merck Research Laboratories
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
China Pharmaceutical University
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Pfizer
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Genentech
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.
Japan Tobacco
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.
East China University of Science & Technology
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.
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.
Takeda Pharmaceutical
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.
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.
Pfizer
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.
Gvk Biosciences
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
Chia Tai Tianqing Pharmaceutical Group
Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34.
Brigham Young University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.
China Pharmaceutical University
The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors.
Hungarian Academy of Sciences
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.
Glaxosmithkline R&D
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.
Gwangju Institute of Science and Technology (Gist)
Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3.
Astellas Pharma
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.
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).
Pfizer
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Janssen Research and Development
Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.
China Pharmaceutical University
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
TBA
The Exploration of Chirality for Improved Druggability within the Human Kinome.
University of Arkansas For Medical Sciences
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.
Eberhard Karls University T£Bingen
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
Shandong University
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
Arromax Pharmatech
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.
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.
Central China Normal University
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.
Southeast University
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Bristol-Myers Squibb
Kinase Chemodiversity from the Arctic: The Breitfussins.
Uit - The Arctic University of Norway
Targeting the immunity protein kinases for immuno-oncology.
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.
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.
West China Hospital of Sichuan University
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.
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.
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.
Novartis Institutes For Biomedical Research
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.
Shanghai Pharmaceuticals Holding
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
National University of Singapore
Design and synthesis of potent RSK inhibitors.
Novartis Institutes For Biomedical Research
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.
Purdue University
Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.
Astellas Pharma
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.
China Pharmaceutical University
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.
Seoul National University
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
Advinus Therapeutics
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.
Second Military Medical University
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Astrazeneca
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.
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.
Sichuan University and Collaborative Innovation Center
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of highly potent, selective, covalent inhibitors of JAK3.
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.
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.
Merck
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
National University of Singapore
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.
Pfizer
Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.
Yale University
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.
Therachem Research Medilab (India)
SUBSTITUTED OXOPYRIDINE DERIVATIVES FOR THE TREATMENT AND/OR PROPHYLAXIS OF THROMBOTIC OR THROMBOEMBOLIC DISORDERS AND/OR THROMBOTIC OR THROMBOEMBOLIC COMPLICATIONS
Bayer Aktiengesellschaft
GONADOTROPIN-RELEASING HORMONE ANTAGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Shandong Luye Pharmaceutical
CONJUGATES COMPRISING ANTIFUNGALS AND HEAT SHOCK PROTEIN 90 (HSP90) INHIBITORS AND METHODS OF USE THEREOF
Bright Angel Therapeutics
ASYMMETRIC BIS-BENZIMIDAZOLE STING AGONIST IMMUNOCONJUGATES AND USES THEREOF
Bolt Biotherapeutics
AROYL SUBSTITUTED TRICYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
Genfleet Therapeutics (Shanghai)
NOVEL PARP7 INHIBITOR AND USE THEREOF
Shanghai Qilu Pharmaceutical Research And Development Centre
INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE, COMPOSITIONS, AND METHODS OF USE
Bristol-Myers Squibb
Substituted phenyloxazolidinones for antimicrobial therapy
The Global Alliance For Tb Drug Development
CARBORANE HYDROXAMIC ACID MATRIX METALLOPROTEINASE INHIBITORS AND AGENTS FOR BORON NEUTRON CAPTURE THERAPY
Loyola University Of Chicago
SALT OF COMPOUND FOR DEGRADING BTK, CRYSTAL FORM THEREOF, AND USE THEREOF IN MEDICINE
Haisco Pharmaceuticals
4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as CDK inhibitors
Carrick Therapeutics
COMPOSITIONS AND METHODS FOR THE PREVENTION AND/OR TREATMENT OF MITOCHONDRIAL DISEASE, INCLUDING FRIEDREICH'S ATAXIA
Stealth Biotherapeutics
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
Benzenesulfonylbenazamide compound for inhibiting BCL-2 protein and composition and use thereof
Shenzhen Targetrx
Heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
Hoffmann-La Roche
Inhibitors of receptor interacting protein kinase I for the treatment of disease
University Of Texas
C-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same
The United States of America, As Represented By The Secretary, Department of Health and Human Services
RIP1 inhibitory compounds and methods for making and using the same
Rigel Pharmaceuticals
Class of amino-substituted nitrogen-containing fused ring compounds, preparation method therefor, and use thereof
Shanghai Ringene Biopharma
Aminopyrimidine compound and composition comprising same and use thereof
Shenzhen Targetrx
Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases
University of Washington Through Its Center For Commercialization
Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof
Merck Sharp & Dohme
Crystal form of urate transporter 1 inhibitor and preparation method and use thereof
Tianjin Institute of Pharmaceutical Research
Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient
Korea Research Institute of Chemical Technology
Imidazopiperazine inhibitors of transcription activating proteins
University Of Texas
Selective inhibitors of Alpha2-containing isoforms of Na,K-ATPase and use thereof for reduction of intraocular pressure
Yeda Research and Development
Benzyl phenyl ether derivative, preparation method therefor, and pharmaceutical composition and uses thereof
Institute of Materia Medica, Chinese Academy of Medical Sciences
Imidazopiperazinone inhibitors of transcription activating proteins
University Of Texas
Substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs
Bayer Pharma Aktiengesellschaft
6-membered heterocyclic derivatives and pharmaceutical composition comprising the same
Shionogi
Pyridinylmethyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases
University of Washington Through Its Center For
Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
Neomed Institute
Methyl- and trifluromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof
Pfizer
Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
Mitobridge
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR
Pfizer
Inhibitors of ACK1/TNK2 tyrosine kinase
H. Lee Moffitt Cancer Center and Research Institute
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International
[1,2,3]triazolo[4,5-D]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor
Hoffmann-La Roche
Matrix metalloproteinase inhibitors and methods for the treatment of pain and other diseases
TBA
Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.
Nas of Ukraine
N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides as androgen receptor antagonists, production and use thereof as medicinal products
Bayer Pharma Aktiengesellschaft
1-[m-carboxamido(hetero)aryl-methyl]-heterocyclyl-carboxamide derivatives
Actelion Pharmaceuticals
Synthesis and structure-activity relationship of novel conformationally restricted analogues of serotonin as 5-HT6 receptor ligands.
Suven Life Sciences
Biphenyl-ethyl-pyrrolidine derivatives as histamine H3 receptor modulators for the treatment of cognitive disorders
Arena Pharmaceuticals
Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors
Washington University
Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.
University of Texas Southwestern Medical Center
Rapid Discovery of Potent and Selective Glycosidase-Inhibiting De Novo Peptides.
The University of Tokyo
Pyrazole and imidazole derivatives useful as orexin antagonists
Actelion Pharmaceuticals
Urea derivatives and their use as fatty-acid binding protein (FABP) inhibitors
Hoffmann-La Roche
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Abbvie
Trifluoromethyl pyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof
Lycera
Novel 1,3,4-oxadiazole/oxime hybrids: Synthesis, docking studies and investigation of anti-inflammatory, ulcerogenic liability and analgesic activities.
Minia University
Histone deacetylase 6 structure and molecular basis of catalysis and inhibition
University of Pennsylvania
In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase.
Universiti Teknologi Mara (Uitm)
Processes for the preparation of (R)-2-(7-4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[B]indol-3-yl)acetic acid and salts thereof
Arena Pharmaceuticals
Substituted azoanthracene derivatives and intermediates for preparation thereof
Vtv Therapeutics
Oxidated derivatives of triazolylpurines useful as ligands of the adenosine A2A receptor and their use as medicaments
Sigma-Tau Industrie Farmaceutiche Riunite
Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities
Deciphera Pharmaceuticals
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies
Galderma Research & Development
Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.
Nanjing University
Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Methods for treating or preventing cancer and neurodegenerative diseases
Sloan-Kettering Institute For Cancer Research
Structure-guided design of a high affinity inhibitor to human CtBP.
University of Massachusetts Medical School
Tetrahydrocyclopenta[c]acridine derivatives as kinase inhibitors and biological
Centre National De La Recherche Scientifique
Synthesis and molecular modelling studies of novel sulphonamide derivatives as dengue virus 2 protease inhibitors.
Birla Institute of Technology
Aminoheteroaryl compounds and preparation method and use thereof
Shanghai Allist Pharmaceuticals
Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease
Merck Sharp & Dohme
Inhibitors of epoxide hydrolases for the treatment of inflammation
University of California
Methods for increasing the stabilization of hypoxia inducible factor-1 alpha
Aerpio Therapeutics
Identification of dipeptidyl peptidase IV inhibitors: virtual screening, synthesis and biological evaluation.
China Pharmaceutical University
Modified macrophage migration inhibitory factor inhibitors
The Feinstein Institute For Medical Research
Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Vitae Pharmaceuticals
Role of the four conserved histidine residues in the amidotransferase domain of carbamoyl phosphate synthetase.
Texas A&M University
Pentachlorophenol hydroxylase, a poorly functioning enzyme required for degradation of pentachlorophenol by Sphingobium chlorophenolicum.
University of Colorado Boulder
Discovery of a Novel Allosteric Modulator of 5-HT3 Receptors: INHIBITION AND POTENTIATION OF CYS-LOOP RECEPTOR SIGNALING THROUGH A CONSERVED TRANSMEMBRANE INTERSUBUNIT SITE.
University of Copenhagen
[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Johnson and Johnson Pharmaceutical Research and Development, Beerse
Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.
Glaxo Group Research
Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism.
Ohio State University
Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.
R. W. Johnson Pharmaceutical Research Institute
Cloning and expression of a 5-hydroxytryptamine7 receptor positively coupled to adenylyl cyclase.
Syntex Discovery Research
Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling.
University of Illinois At Chicago
1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain.
Stanford University
Cloning and expression of an A1 adenosine receptor from rat brain.
National Institute of Mental Health
Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.
Duke University