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321 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28249207 78 Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.EBI East China Normal University
28140585 52 Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.EBI High Magnetic Field Laboratory
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
26169764 48 Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.EBI China Pharmaceutical University
28254166 81 Discovery of novel BTK inhibitors with carboxylic acids.EBI Merck & Co. Inc
27912175 14 Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.EBI Dalian Medical University
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
27956037 8 Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.EBI Dalian Medical University
27994757 41 Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.EBI Pvt. Ltd.
27994736 28 Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing aEBI Dalian Medical University
27583770 82 Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two LockeEBI Bristol-Myers Squibb Research and Development
27288183 130 Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI Southeast University
27210433 10 Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.EBI China Pharmaceutical University
26976214 15 Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.EBI KBP Biosciences
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26762835 342 Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).EBI Icahn School of Medicine at Mount Sinai
26630553 9 Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.EBI Chinese Academy of Sciences
26675441 46 Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.EBI Genentech
26396685 19 Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.EBI Amgen Inc
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26320619 88 Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
26344595 26 Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.EBI Xi'an Jiaotong University
26277759 31 Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.EBI China Pharmaceutical University
26258521 104 Development of Selective Covalent Janus Kinase 3 Inhibitors.EBI Harvard Medical School
26087137 30 Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.EBI Takeda California Inc
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc
25835317 63 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.EBI Sichuan University
25872980 21 TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.EBI Carna Biosciences, Inc
25701252 54 Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.EBI Genentech
25596757 64 Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.EBI China Pharmaceutical University
25630223 5 Target engagement in lead generation.EBI Eli Lilly and Company
25589924 6 Novel Disubstituted Pyrimidines as Inhibitors of Bruton's Tyrosine Kinase.EBI Dart Neuroscience LLC
25515957 33 Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.EBI China Pharmaceutical University
25466710 14 Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.EBI Hoffmann-La Roche Inc
24915291 73 Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.EBI Peking University
24731277 2 Small chemicals with inhibitory effects on PtdIns(3,4,5)P3 binding of Btk PH domain.EBI Konkuk University
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
24900590 55 Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.EBI GlaxoSmithKline
23742252 81 Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase EBI Genomics Institute of the Novartis Research Foundation
23442188 4 A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.EBI Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc
21429745 49 3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.EBI GlaxoSmithKline
22621397 39 Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI Covalution Pharma BV
22726925 216 Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI Cellzome Ltd
23098091 91 Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.EBI Pfizer Inc
24900538 27 Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.EBI TBA
22394077 19 Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.EBI Hoffmann-La Roche Inc
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc
22148921 48 Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-cEBI Cephalon Inc
19716697 110 The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.EBI Boehringer Ingelheim Pharmaceuticals Inc
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
18321716 7 ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.EBI Institute of Molecular Physiology
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
17684099 4 The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.EBI Center for Molecular Medicine of the Austrian Academy of Sciences
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18278858 93 Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer Inc
22014550 337 Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI Ansaris
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Rhône-Poulenc Rorer
21958547 108 Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.EBI Pfizer Inc
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21936542 143 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI Novartis Institute for BioMedical Research
21733693 7 Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.EBI GlaxoSmithKline
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer Inc
21391610 139 Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI Vertex Pharmaceuticals Inc
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
19039322 50 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.EBI Center for Molecular Medicine of the Austrian Academy of Sciences
20307980 22 B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI Wyeth Research
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
19362830 47 Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI Wyeth Research
19019675 52 Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?EBI Pfizer Inc
18993068 75 Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.EBI Amgen Inc
18667312 24 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.EBI The Scripps Research Institute
17499505 78 Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.EBI Boehringer Ingelheim Pharmaceuticals Inc
17350837 59 Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI Amgen Inc
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc
16686533 89 Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.EBI Boehringer Ingelheim Pharmaceuticals Inc
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc
32832028 47 Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.EBI Genentech
30893553 62 Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).EBI Bristol-Myers Squibb Research and Development
31866272 17 Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.EBI Dalian Medical University
31879210 2 Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.EBI Yale University
31843459 57 Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.EBI Chia Tai Tianqing Pharmaceutical Group Co., Ltd
31830635 74 Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI Peking University
31757666 314 Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI Merck & Co.
27491711 422 Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI Merck and Co.
27429068 54 Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.EBI GlaxoSmithKline R&D
27578246 158 Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.EBI GlaxoSmithKline R&D
27531604 55 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).EBI Bristol-Myers Squibb Research and Development
30605829 24 Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3K?.EBI China Pharmaceutical University
31381333 302 Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI TBA
30562697 84 The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.EBI University of Silesia in Katowice
31221612 20 Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.EBI East China University of Science & Technology
31138459 50 Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.EBI Biogen Inc.
30655951 83 Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.EBI Pfizer Inc.
30532965 81 Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.EBI GlaxoSmithKline R&D
29522671 80 Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.EBI Chinese Academy of Sciences
28528303 171 Discovery of a potent dual ALK and EGFR T790M inhibitor.EBI Harvard Medical School
31693351 473 Discovery of 4EBI TBA
31368705 57 Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.EBI Merck KGaA
30522954 11 Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.EBI Shanghai Institute of Pharmaceutical Industry
31234030 38 Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.EBI Nankai University
32083858 145 Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI TBA
31550151 17 The Exploration of Chirality for Improved Druggability within the Human Kinome.EBI University of Arkansas for Medical Sciences
30939001 1 Synthetic Approaches to the New Drugs Approved During 2017.EBI Seattle Genetics, Inc.
31103903 47 Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.EBI China Pharmaceutical University
30565923 34 Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.EBI Eberhard Karls University T£bingen
31395509 43 Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.EBI Peking University Health Science Center
31077998 81 Targeting tropomyosin receptor kinase for cancer therapy.EBI China Pharmaceutical University
30999237 90 Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).EBI Peking University
30927566 52 Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.EBI Shenyang Pharmaceutical University
30875504 34 Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.EBI Sichuan University and Collaborative Innovation Center
31260299 14 Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.EBI Tsinghua University
30508668 62 Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation.EBI China Pharmaceutical University
30384048 365 ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI University of Florida
30343954 16 Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.EBI Eppley Institute for Research in Cancer and Allied Diseases
31526603 379 Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI Takeda Pharmaceutical Company Limited
30857748 1 Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.EBI Shandong University
30857747 8 A potent seven-membered cyclic BTK (Bruton's tyrosine Kinase) chiral inhibitor conceived by structure-based drug design to lock its bioactive conformation.EBI Hoffmann-La Roche Ltd.
28139931 85 Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.EBI Pfizer Inc.
26505898 123 Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI Novartis Institutes for Biomedical Research
26509640 234 Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI AbbVie Bioresearch Center
28986130 11 Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents.EBI Dalian Medical University
30423248 226 Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.EBI Pfizer Inc.
30290988 31 Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.EBI EMD Serono Research & Development Institute, Inc.
30243592 23 Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.EBI EMD Serono Research & Development Institute, Inc.
30480444 85 Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.EBI Sichuan University/Collaborative Innovation Center of Biotherapy
29146136 32 Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.EBI The First Affiliated Hospital of Dalian Medical University
30139575 98 Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.EBI China Pharmaceutical University
30122225 25 Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.EBI EMD Serono Research & Development Institute, Inc.
30097367 96 Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.EBI Bristol-Myers Squibb Company
30082069 359 ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI Vertex Pharmaceuticals Inc
30077608 24 Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3K?.EBI China Pharmaceutical University
30006143 14 Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.EBI Dalian Medical University
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals, Inc
29567295 19 Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors.EBI Shanghai Institute of Pharmaceutical Industry
30216722 77 Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.EBI Carna Biosciences, Inc.
30034582 72 Covalent Inhibitors of the TEC Family of Kinases and Their Methods of Use.EBI Temple University School of Pharmacy
28947935 5 Bruton's Tyrosine Kinase Inhibitors for the Treatment of Autoimmune Diseases and Cancers.EBI AMRI
28131712 30 Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).EBI Integral BioSciences, Pvt. Ltd.
29715023 56 Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.EBI China Pharmaceutical University
29198867 46 Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.EBI Carna Biosciences, Inc.
28279528 53 Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.EBI Advinus Therapeutics Ltd
29631132 33 The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.EBI Shaanxi University of Science & Technology
29107425 90 Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI Korea Institute of Science and Technology (KIST)
28628824 98 Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.EBI University of Science and Technology of China
29852068 86 Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.EBI Eberhard Karls University T£bingen
28734581 37 Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.EBI Sichuan University and Collaborative Innovation Center
28720503 146 Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.EBI Merck & Co.
28432946 13 Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.EBI Dalian Medical University
28282122 9 Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.EBI High Magnetic Field Laboratory
28259529 31 Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI The Ohio State University
28927786 52 Discovery of highly potent, selective, covalent inhibitors of JAK3.EBI Bristol-Myers Squibb Research and Development
28337328 6 Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.EBI Dana-Farber Cancer Institute Inc
28626519 48 Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.EBI Genentech
28438385 24 Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth.EBI Indiana University School of Medicine
28956923 34 Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.EBI Chinese Academy of Sciences
28408223 5 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.EBI IntelliSyn Pharma
28315597 85 Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.EBI University of Science and Technology of China
29457982 80 Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.EBI Genentech
28945083 33 In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.EBI National Institute of Biological Sciences, Beijing
28433531 69 Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.EBI WuXi AppTec (Shanghai) Co. Ltd
34414360 60 Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.BDB The University of Arizona
 9 Inhibition of SARS-CoV-2 main protease by allosteric drug-bindingBDB Center for Free-Electron Laser Science
33283984 11 A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease InhibitorsBDB Texas A&M University
21612376 6 Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine.BDB GITAM University
21438710 18 Oxamic acid analogues as LDH-C4-specific competitive inhibitors.BDB Instituto Politécnico Nacional
24047900 19 Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.BDB Vanderbilt University
20962348 17 Probing the active site of the deoxynucleotide N-hydrolase Rcl encoded by the rat gene c6orf108.BDB Institut Pasteur
14564311 4 Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.BDB University of Maryland Hospital
11303063 11 Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.BDB Creighton University
10374926 2 Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.BDB Hungarian Academy of Sciences
9081563 67 Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.BDB TBA
8996185 121 Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.BDB Synthélabo Recherche
8394362 99 Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.BDB National Institute of Neurological Disorders and Stroke
15696597 18 Structure-aided optimization of kinase inhibitors derived from alsterpaullone.BDB Technische Universität Braunschweig
8234299 8 Molecular cloning and characterization of the human A3 adenosine receptor.BDB Merck Research Laboratories
8102973 31 Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications.BDB Maryland Psychiatric Research Center
7996470 29 The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.BDB University of Michigan
2968449 13 Characterization of [5,6-3H]SQ 29,548 as a high affinity radioligand, binding to thromboxane A2/prostaglandin H2-receptors in human platelets.BDB Squibb Institute for Medical Research
2419545 57 Characterization and autoradiographic localization of multiple tachykinin binding sites in gastrointestinal tract and bladder.BDB National Institutes of Health
2139469 31 Characterization of D1 dopamine receptors in the bovine pineal gland with [3H]SCH 23390.BDB University of Nebraska
18804036 24 Structure-guided development of efficacious antifungal agents targeting Candida glabrata dihydrofolate reductase.BDB University of Connecticut
15293988 1 A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.BDB Virginia Commonwealth University
18722768 10 Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.BDB Anadys Pharmaceuticals
18242088 26 Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.BDB Anadys Pharmaceuticals
19477642 87 Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.BDB GSK
19167883 5 Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.BDB Gilead Sciences Inc
19071019 16 Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors.BDB Roche
18290603 5 Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase.BDB Vertex Pharmaceuticals Inc
15857113 12 Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.BDB GSK
17709247 33 Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.BDB Amgen Inc
15755665 7 Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.BDB Pfizer Inc
17114291 10 Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.BDB Johns Hopkins University
17636946 94 Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.BDB GSK
15466206 10 BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.BDB Bayer Pharmaceuticals Corporation
17523610 73 Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.BDB Abbott Laboratories
15582402 9 Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).BDB University of Illinois at Chicago
17451235 19 Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.BDB Astex
14592490 80 Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.BDB Merck Research Laboratories
16942016 27 Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.BDB University of Kansas
15887974 10 Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.BDB Universidad Central de Venezuela
15537349 18 Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.BDB University of Bologna
10866371 12 Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.BDB GlaxoSmithKline
15743198 134 Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.BDB Saarland University
16392787 16 Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.BDB Burnham Institute
11266159 63 3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).BDB SmithKline Beecham Pharmaceuticals Ltd
15771433 30 Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.BDB Johnson & Johnson Pharmaceutical
8568816 69 Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor ReceptorBDB Parke-Davis Pharmaceutical Research
8642565 36 Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.BDB Sandoz Research Institute
 50 Potent, orally bioavailable HIV-1 protease inhibitors containing noncoded D-amino acidsBDB Eli Lilly and Company
8558507 7 A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.BDB Abbott Laboratories