405 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China Normal University
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Principia Biopharma
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National University of Singapore
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kasetsart University
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda California
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Central China Normal University
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dalian Medical University
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Auckland
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southeast University
Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Konkuk University
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shandong University
Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kangwon National University
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb R & D
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research & Development
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shandong University
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xi'An Jiaotong University
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hoffmann-La Roche
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Syncom
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Lexicon Pharmaceuticals
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Galapagos
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peking University
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Toronto
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Fox Chase Chemical Diversity Center
Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Konkuk University
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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 ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genomics Institute of The Novartis Research Foundation
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hoffmann-La Roche
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
F. Hoffmann-La Roche
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
F. Hoffmann-La Roche
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
S*Bio
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Argenta Discovery
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
S Bio
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca R&D
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sri International
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Frosst Centre For Therapeutic Research
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Procter and Gamble Pharmaceuticals
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Procter and Gamble Pharmaceuticals
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Kentucky
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ludwig-Maximilians University of Munich
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ansaris
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RhôNe-Poulenc Rorer
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute For Biomedical Research
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ariad Pharmaceuticals
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca R&D Boston
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
5-amino-pyrazoles as potent and selective p38a inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences Oncology
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Université
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute of Biomedical Research
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ligand Pharmaceuticals
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca R&D Boston
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Human Genome Research Institute
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The Scripps Research Institute
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Simplified staurosporine analogs as potent JAK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharmaceutical Research Institute
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Bioresearch Center
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Aventis Pharmaceuticals
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japan Tobacco
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science & Technology
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Strathclyde
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shenyang Pharmaceutical University
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dalian Medical University
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Gvk Biosciences
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chia Tai Tianqing Pharmaceutical Group
Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peking University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck And
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline R&D
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Gwangju Institute of Science and Technology (Gist)
Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Janssen Research and Development
Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline R&D
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
The Exploration of Chirality for Improved Druggability within the Human Kinome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Arkansas For Medical Sciences
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard Karls University T£Bingen
Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peking University
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shandong University
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University and Collaborative Innovation Center
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Arromax Pharmatech
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science & Technology
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Central China Normal University
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southeast University
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peking University
Targeting the immunity protein kinases for immuno-oncology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Florida
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
West China Hospital of Sichuan University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universitaire Vaudois
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National University of Singapore
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Purdue University
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Yunnan University
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Beijing Normal University
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The First Affiliated Hospital of Dalian Medical University
Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dalian Medical University
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Seoul National University
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard-Karls-University Tuebingen
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Advinus Therapeutics
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shaanxi University of Science & Technology
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Second Military Medical University
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science & Technology (Kist)
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Science and Technology of China
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard Karls University T£Bingen
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University and Collaborative Innovation Center
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The Ohio State University
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Discovery of highly potent, selective, covalent inhibitors of JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National University of Singapore
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Science and Technology of China
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Therachem Research Medilab (India)
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Moffitt Cancer Center
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wuxi Apptec (Shanghai)
A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
A*Star
Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nas of Ukraine
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Centre De Recherche De Gif
Fatty acid-binding protein 5 (FABP5) regulates cognitive function both by decreasing anandamide levels and by activating the nuclear receptor peroxisome proliferator-activated receptor ß/d (PPARß/d) in the brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Case Western Reserve University School of Medicine
Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Griffith University
Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Panjab University
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Takeda Chemical Industries
Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Creighton University
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Colorado
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
F. Hoffmann-La Roche
High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nankai University
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
National Institute of Mental Health
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cyclacel
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Yale University
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Universita Del Piemonte Orientale
Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Gilead Sciences
Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
The Johns Hopkins University
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Gsk
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Astrazeneca
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Lund University
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Morphochem
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Johns Hopkins University
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Illinois At Chicago
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Axys Pharmaceutical
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Glaxosmithkline
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Glaxosmithkline
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Istituto Di Cristallografia
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Bologna
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Wyeth-Ayerst Research