488 articles for thisTarget
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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.
East China Normal University
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Sichuan University And Collaborative Innovation Center For Biotherapy
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
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
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.
National University Of Singapore
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.
Kasetsart University
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.
Central China Normal University
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
University Of Nebraska Medical Center
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
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.
Nerviano Medical Sciences
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.
Shandong University
Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.
China Pharmaceutical University
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Genentech
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Merck
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.
Takeda Pharmaceutical
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).
Icahn School Of Medicine At Mount Sinai
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
Kangwon National University
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Bristol-Myers Squibb R & D
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Bristol-Myers Squibb Research & Development
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.
Shandong University
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.
Xi'An Jiaotong University
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.
China Pharmaceutical University
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Nerviano Medical Sciences
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.
Zhejiang University
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.
Astrazeneca
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
Hoffmann-La Roche
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.
Astellas Pharma
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Bristol-Myers Squibb
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.
Vertex Pharmaceuticals
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute Of The Novartis Research Foundation
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.
Sichuan University
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.
University Of South Florida
Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
Central South University
Discovery and profiling of a selective and efficacious Syk inhibitor.
Novartis Institutes For Biomedical Research
Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.
Nerviano Medical Sciences
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Vertex Pharmaceuticals
Computer-aided discovery of aminopyridines as novel JAK2 inhibitors.
Chonnam National University
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.
Pfizer
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.
Syncom
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Bristol-Myers Squibb
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Genentech
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Galapagos
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Novartis Institutes For Biomedical Research
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Pfizer
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Gilead Sciences
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Bristol-Myers Squibb Research And Development
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.
Merck
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.
Merck
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.
University Of Zurich
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Pfizer
A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.
University Of Toronto
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.
Fox Chase Chemical Diversity Center
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.
Zhejiang University
Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.
University Of Zurich
Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.
Konkuk University
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
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
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.
Merck Research Laboratories
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.
Astrazeneca
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.
Hoffmann-La Roche
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
F. Hoffmann-La Roche
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Design and synthesis of tricyclic cores for kinase inhibition.
Abbott Bioresearch Center
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
F. Hoffmann-La Roche
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Glaxosmithkline
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Exelixis
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph
S*Bio
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Sichuan University
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Genentech
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.
Genentech
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Genentech
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.
Exelixis
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
TBA
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Argenta Discovery
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.
Janssen Pharmaceutical Companies Of Johnson & Johnson
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.
Cephalon
Structure-based optimization of aminopyridines as PKC¿ inhibitors.
Vertex Pharmaceuticals
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
Hanmi Research Center
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth
S Bio
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Astrazeneca R&D Boston
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Merck Research Laboratories
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
Novartis Institutes For Biomedical Research
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Astrazeneca R&D
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.
Merck Research Laboratories
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
Sri International
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Vertex Pharmaceuticals
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Nerviano Medical Sciences
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Vertex Pharmaceuticals
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.
Amgen
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Merck Frosst Centre For Therapeutic Research
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).
Procter And Gamble Pharmaceuticals
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.
Procter And Gamble Pharmaceuticals
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase
S Bio
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Ludwig-Maximilians University Of Munich
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.
Amgen
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.
Cephalon
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.
Nerviano Medical Sciences
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Cephalon
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Vertex Pharmaceuticals
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Merck
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Novartis Institute For Biomedical Research
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Astrazeneca R&D Boston
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.
Abbott Laboratories
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
Bristol-Myers Squibb
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
Abbott Laboratories
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.
Pfizer
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Nerviano Medical Sciences Oncology
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Université
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Novartis Institute Of Biomedical Research
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Abbott Laboratories
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Novartis Institutes For Biomedical Research
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.
Novartis Institutes For Biomedical Research
Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.
Astrazeneca R&D Boston
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Novartis Institutes For Biomedical Research
2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.
Ligand Pharmaceuticals
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.
Vertex Pharmaceuticals
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.
Astrazeneca R&D Boston
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Vertex Pharmaceuticals
Design and synthesis of a novel tyrosine kinase inhibitor template.
St. Jude Children'S Research Hospital
Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening.
Semmelweis University
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Astrazeneca R&D Boston
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).
National Human Genome Research Institute
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.
Astrazeneca Pharmaceuticals
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Amgen
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute Of The Novartis Research Foundation
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.
University Of Oklahoma Health Sciences Center
Entry into a new class of protein kinase inhibitors by pseudo ring design.
Novartis Institutes For Biomedical Research
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Amgen
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Amgen
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Cyclic mimetics of kinase-inhibitory region of Suppressors of Cytokine Signaling 1: Progress toward novel anti-inflammatory therapeutics.
University Of Naples "Federico Ii
Discovery and optimization of selective RET inhibitors via scaffold hopping.
Guangzhou Baiyunshan Pharmaceutical Holdings
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-
The Genomics Institute Of The Novartis Research Foundation
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
Design, synthesis, and biological evaluation of 2,4-diamino pyrimidine derivatives as potent FAK inhibitors with anti-cancer and anti-angiogenesis activities.
Guizhou Medical University
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.
University Of Chinese Academy Of Science
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
Aventis Pharmaceuticals
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
China Pharmaceutical University
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Ontario Institute For Cancer Research
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Incyte
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
Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
Sichuan University
Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives.
University Bangkok
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
Chinese Academy Of Sciences
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
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Vertex Pharmaceuticals
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Roche Innovation Center Shanghai
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Moffitt Cancer Center
Design, synthesis, biological activity evaluation of 3-(4-phenyl-1H-imidazol-2-yl)-1H-pyrazole derivatives as potent JAK 2/3 and aurora A/B kinases multi-targeted inhibitors.
Xuzhou Medical University
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Biogen
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.
Newcastle University
Discovery of a novel kinase hinge binder fragment by dynamic undocking.
Universitat De Barcelona
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 a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.
Vertex Pharmaceuticals
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Pfizer
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Bristol Myers Squibb Research
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
Chimeric Peptidomimetics of SOCS 3 Able to Interact with JAK2 as Anti-inflammatory Compounds.
University Of Naples "Federico Ii
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
Efficacy and Tolerability of Pyrazolo[1,5-
The Genomics Institute Of The Novartis Research Foundation
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Gilead Sciences
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? 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
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
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
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
Bristol-Myers Squibb Research And Development
Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor.
Virginia Tech
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
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Vertex Pharmaceuticals
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.
Glaxosmithkline R&D
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
TBA
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Shenyang Pharmaceutical University
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
Yale University
The Exploration of Chirality for Improved Druggability within the Human Kinome.
University Of Arkansas For Medical Sciences
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.
Vertex Pharmaceuticals (Europe)
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.
Eberhard Karls University T£Bingen
Targeting tropomyosin receptor kinase for cancer therapy.
China Pharmaceutical University
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.
Shenyang Pharmaceutical University
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
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
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
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 A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.
Nerviano Medical Sciences
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Moffitt Cancer Center
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
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Glaxosmithkline R&D
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
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.
Bristol-Myers Squibb
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
National University Of Singapore
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).
National University Of Singapore
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
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
Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
University Of Sharjah
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.
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.
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
Drug Discovery Targeting Bromodomain-Containing Protein 4.
University Of Texas Medical Branch
Natural-Based Indirubins Display Potent Cytotoxicity toward Wild-Type and T315I-Resistant Leukemia Cell Lines.
Beckman Research Institute
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
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.
Yale University
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.
Therachem Research Medilab (India)
Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.
Martin-Luther-University Halle-Wittenberg
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.
Moffitt Cancer Center
A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.
A*Star
Inhibition of acetylpolyamine and spermine oxidases by the polyamine analogue chlorhexidine.
University Roma Tre
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.
Centre De Recherche De Gif
Fatty acid-binding protein 5 (FABP5) regulates cognitive function both by decreasing anandamide levels and by activating the nuclear receptor peroxisome proliferator-activated receptor ß/d (PPARß/d) in the brain.
Case Western Reserve University School Of Medicine
Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.
Griffith University
Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.
Panjab University
Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation.
Mcgill University
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.
Aimst University
Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A.
University Of Kentucky
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.
I.G.B.M.C.
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.
Takeda Chemical Industries
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.
University Of Colorado
PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.
Pharmacia & Upjohn
Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, a new uptake inhibitor with selectivity for serotonin.
Pfizer
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.
Cyclacel
Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts.
Universitat De Barcelona
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.
Boehringer Ingelheim Pharmaceuticals
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Yale University
Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Amgen
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.
Acadia Pharmaceuticals
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).
University Of Michigan
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.
Cephalon
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.
Astrazeneca
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.
Lund University
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.
Morphochem
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.
Johns Hopkins University
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
Gsk
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).
University Of Illinois At Chicago
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Axys Pharmaceutical
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
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.
Glaxosmithkline
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Pfizer
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
Istituto Di Cristallografia
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
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.
University Of Bologna
Identification of potent and novel small-molecule inhibitors of caspase-3.
Sunesis Pharmaceuticals
3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).
Smithkline Beecham Pharmaceuticals
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
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.
Merck Research Laboratories