382 articles for thisTarget

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PMID	Data	Article Title	Organization
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
28109791	44	Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.	Chugai Pharmaceutical
27966954	19	Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.	High Magnetic Field Laboratory
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27994749	47	Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.	Astrazeneca
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 Locke	Bristol-Myers Squibb Research and Development
27299736	37	The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.	St. John'S University
27491023	286	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.	University of Auckland
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27010810	24	Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.	Oribase Pharma
27003761	120	Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.	Nerviano Medical Sciences
26951750	59	Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.	Novartis Institutes For Biomedical Research
26951753	336	Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.	Novartis Institutes For Biomedical Research
26713112	36	Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.	Genentech
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).	Icahn School of Medicine At Mount Sinai
26475520	43	Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.	Korea University of Science and Technology (Ust)
26396681	58	Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.	Novartis Institutes For Biomedical Research
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26320619	88	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
26288682	64	Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.	Bristol-Myers Squibb Research & Development
26222319	192	Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.	Nerviano Medical Sciences
26087137	30	Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.	Takeda California
26005534	158	(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.	Genomics Institute of The Novartis Research Foundation
25844760	52	Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.	Genentech
25699576	42	Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.	University of South Florida
25089810	79	Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.	National Taiwan University
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24913714	53	Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.	Merck Research Laboratories
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
25369270	93	Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.	Galapagos
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
25221654	39	Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.	Novartis Institutes For Biomedical Research
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24915291	73	Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.	Peking University
24904961	27	Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.	Qilu Pharmaceutical
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	Takeda Pharmaceutical
23434140	35	Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.	East China University of Science and Technology
23301767	154	Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.	University of Nottingham
23362959	72	Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.	Sichuan University
23253074	38	Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.	University of Zurich
23398373	88	Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.	Vertex Pharmaceuticals
23312943	166	Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
23312472	129	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
23273517	53	Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.	National Center For Advancing Translational Sciences
10741557	26	Naphthyl ketones: a new class of Janus kinase 3 inhibitors.	Astrazeneca
22929232	89	Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.	Amgen
21903390	79	Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.	Glaxosmithkline
19303774	87	1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.	Glaxosmithkline
19427202	8	Natural product inhibitors of protein-protein interactions mediated by Src-family SH2 domains.	Max Planck Institute of Biochemistry
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.	Cellzome
23098265	46	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.	University of Genoa
22827572	67	Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).	Glaxosmithkline
22734674	81	The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.	Amgen
22257213	98	Discovery and development of spleen tyrosine kinase (SYK) inhibitors.	Rigel
22746295	91	Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.	Teijin Pharma
22039836	188	Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).	Johnson & Johnson Pharmaceutical Research & Development
24900387	11	Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.	TBA
22980219	55	Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.	Takeda Pharmaceutical
22695126	98	Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.	Abbott Laboratories
22320388	116	Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.	University of Washington
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
24900482	32	Targeted kinase selectivity from kinase profiling data.	TBA
22738630	76	Structure-based optimization of aminopyridines as PKC¿ inhibitors.	Vertex Pharmaceuticals
22452518	22	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.	Sichuan University
22439974	79	Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.	Takeda Pharmaceutical
22404346	52	Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.	The Institute of Cancer Research
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen
22168626	32	Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.	Ambit Biosciences
22503250	128	Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.	Amri
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
22464456	27	X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.	Sanofi Us
24900358	69	Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.	TBA
21128646	88	Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.	Merck Research Laboratories
15975507	13	Features of selective kinase inhibitors.	University of California San Francisco
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20153204	109	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
20038108	19	Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.	Wyeth Research
19703774	56	C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.	Wyeth Research
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19610618	41	Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.	University of South Florida
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19522465	102	Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).	Boehringer Ingelheim Pharma
19320489	125	Discovery and development of aurora kinase inhibitors as anticancer agents.	Vertex Pharmaceuticals
14593182	34	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.	Pfizer
18789685	172	Kinase array design, back to front: biaryl amides.	Glaxosmithkline
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18434148	43	Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.	Wyeth Research
18395443	37	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.	Bristol-Myers Squibb
17371799	12	Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr	Targegen
17360485	10	Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.	Millennium Pharmaceuticals
18359226	50	Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.	Bristol-Myers Squibb Research and Development
18324761	65	Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.	Amgen
18324759	133	Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.	Amgen
18311900	89	Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.	Amgen
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
17997320	29	Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.	Kissei Pharmaceutical
17983756	55	Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.	Osi Pharmaceuticals
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.	Amgen
18271520	423	Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.	University of Zurich
18083554	54	N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.	Amgen
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17887663	34	Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.	Pfizer
17113292	73	Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.	Targegen
17095233	45	Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.	Kissei Pharmaceutical
15115396	112	General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.	Yale University
11931608	17	Inhibition of protein-protein association by small molecules: approaches and progress.	Pfizer
11448224	9	Nonpeptidic, monocharged, cell permeable ligands for the p56lck SH2 domain.	Boehringer Ingelheim (Canada)
10737750	7	SH2-directed ligands of the Lck tyrosine kinase.	The Albert Einstein College of Medicine
10346928	19	Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.	Boehringer Ingelheim Pharmaceuticals
11992778	26	Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.	Roche Products
	48	The preparation and sar of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: Inhibitors of p56lck and EGF-R tyrosine kinase activity	TBA
22310227	89	5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.	Glaxosmithkline
22221201	32	VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.	University of Kentucky
16476733	18	Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.	University of Queensland
22269278	50	Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.	Chugai Pharmaceutical
22136433	67	7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.	Ludwig-Maximilians University of Munich
22154349	123	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
22119469	107	Novel and selective spiroindoline-based inhibitors of Sky kinase.	Pfizer
22101132	41	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.	Shionogi
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).	Ansaris
22003817	71	Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.	Takeda Pharmaceutical
22014755	36	Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.	Hanyang University
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	RhôNe-Poulenc Rorer
21958547	108	Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.	Pfizer
21794960	194	Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.	Universit£
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	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.	Novartis Institute For Biomedical Research
21855335	185	Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.	Merck Research Laboratories
21812414	106	Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).	Pfizer
21536449	16	Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.	The Institute of Cancer Research
21733693	7	Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.	Glaxosmithkline
21705217	60	Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.	Bristol-Myers Squibb
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21493067	22	In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.	Astrazeneca R&D Boston
21470862	110	NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.	Nerviano Medical Sciences
21391610	139	Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.	Vertex Pharmaceuticals
21375264	77	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors	Roche Palo Alto
21341678	49	Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.	Millennium Pharmaceuticals
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21084189	29	Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity.	Institute of Technology and Science
21177105	38	Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Research and Development
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research and Development
20961062	42	Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.	Pfizer
20932747	61	The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.	Ansaris
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20855207	26	Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
19039322	50	Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.	Center For Molecular Medicine of The Austrian Academy of Sciences
18559524	21	BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.	Boehringer Ingelheim Austria
16783341	34	Rational design of inhibitors that bind to inactive kinase conformations.	Novartis Research Foundation
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute of Biomedical Research
20462263	127	Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.	Cyclacel
20459125	60	Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.	Amgen
20397705	208	Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.	Nerviano Medical Sciences
20382527	26	Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.	Bristol-Myers Squibb Research and Development
20346655	117	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
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	Wyeth Research
20218619	44	Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.	Amgen
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	Schering-Plough
20153643	68	Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.	Wyeth Research
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
19854052	420	Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.	Genomics Institute of The Novartis Research Foundation
20148563	42	BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.	The Institute of Cancer Research
20143778	70	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.	Curis
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
20093027	92	Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.	Chugai Pharmaceutical
19945867	39	Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.	Taisho Pharmaceutical
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19762237	58	First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.	Wyeth Research
19682896	49	C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.	Wyeth Research
19674899	54	Disubstituted pyrimidines as Lck inhibitors.	Merck Research Laboratories
19888761	52	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.	Hanmi Research Center
19857964	3	Structural basis for the inhibitor recognition of human Lyn kinase domain.	Osaka Prefecture University
19775160	79	2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.	Takeda Pharmaceutical
19361991	80	Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.	Vertex Pharmaceuticals
19427203	28	Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.	Johnson & Johnson Pharmaceutical Research & Development
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
19572547	51	9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.	Ariad Pharmaceuticals
1479375	215	Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor Agents	TBA
	46	The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-	TBA
	8	Synthesis of a series of brominated 1-phenyl-2-pyridylethenes as inhibitors of the protein-tyrosine kinase p56lck	TBA
	15	Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors	TBA
	34	Synthesis and evaluation of new protein-tyrosine kinase inhibitors. Part 2. Phenylhydrazones.	TBA
	28	Synthesis and evaluation of new protein-tyrosine kinase inhibitors. Part 1. pyridine-containing stilbenes and amides.	TBA
	6	Structural influences of styryl-based inhibitors on epidermal growth factor receptor and p56lck tyrosine-specific protein kinases.	TBA
19447612	59	Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.	Wyeth Research
19394221	2	Application of combinatorial biocatalysis for a unique ring expansion of dihydroxymethylzearalenone.	Amri
19317452	155	Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.	Wyeth Research
19111463	46	Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.	Wyeth Research
19101143	70	Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).	Glaxosmithkline
19053756	27	Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).	National Human Genome Research Institute
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?	Pfizer
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.	Amgen
18977146	2	The importance of CH/pi hydrogen bonds in rational drug design: An ab initio fragment molecular orbital study to leukocyte-specific protein tyrosine (LCK) kinase.	Kissei Pharmaceutical
18817365	73	Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.	Amgen
18799314	8	Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.	Hunter College of Cuny
18793846	33	Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.	Genomics Institute of The Novartis Research Foundation
18723346	26	Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.	Amgen
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	Wyeth Research
18602262	56	Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.	Glaxosmithkline
18585046	32	A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.	Kissei Pharmaceutical
18554909	50	Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.	Amgen
18447379	96	Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.	Amgen
17897956	3	Lateral compartmentalization of T cell receptor versus CD45 by galectin-N-glycan binding and microfilaments coordinate basal and activation signaling.	University of California
16441060	12	A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.	Griffith University
18313298	40	The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.	Bristol-Myers Squibb
18289854	44	Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.	Bristol-Myers Squibb Research and Development
17606372	66	5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Pharmaceutical Research Institute
17425296	161	1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.	Abbott Laboratories
17391959	100	Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.	Abbott Laboratories
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen
17343372	143	Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.	Abbott Laboratories
17280833	52	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
17270437	68	New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Pharmaceutical Research Institute
17234410	82	Discovery of thienopyridines as Src-family selective Lck inhibitors.	Abbott Bioresearch Center
16997556	32	The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).	Procter and Gamble Pharmaceuticals
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
16931012	61	Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.	Targegen
16789733	41	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.	Bristol-Myers Squibb Pharmaceutical Research Institute
16757169	26	The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck).	Procter and Gamble Pharmaceuticals
16750628	47	Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.	Abbott Laboratories
16682201	37	Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.	Procter & Gamble Pharmaceuticals
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16570908	39	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.	Pharmaceutical Research Institute
16516473	444	Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.	Astrazeneca
16366598	51	(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.	Johnson & Johnson Pharmaceutical Research and Development
16216497	67	Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.	Abbott Bioresearch Center
16134929	22	Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.	Bristol-Myers Squibb
15943473	136	Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
15615512	21	Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.	Bristol-Myers Squibb Pharmaceutical Research Institute
15566298	34	The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.	Bristol-Myers Squibb
15214778	8	Identification of non-phosphate-containing small molecular weight inhibitors of the tyrosine kinase p56 Lck SH2 domain via in silico screening against the pY + 3 binding site.	University of Maryland
15109663	26	A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.	Abbott Bioresearch Center
14684325	154	Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.	Sugen
14592495	60	Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).	Bristol-Myers Squibb Pharmaceutical Research Institute
14505648	8	Design and synthesis of small chemical inhibitors containing different scaffolds for lck SH2 domain.	Mogam Biotechnology Research Institute
12941342	21	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
12852972	79	Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
12798323	72	Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.	Bristol-Myers Squibb Pharmaceutical Research Institute
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12482439	51	Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.	Merck Research Laboratories
12372522	51	Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.	Bristol-Myers Squibb Pharmaceutical Research Institute
12217360	27	Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains.	Mogam Biotechnology Research Institute
12139450	29	Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12086485	10	Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.	Boehringer Ingelheim Pharmaceuticals
12039590	51	Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.	Abbott Bioresearch Center
11992777	46	Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).	Bristol-Myers Squibb Pharmaceutical Research Institute
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
11909733	30	Beta-carbolines as specific inhibitors of cyclin-dependent kinases.	Institute of Molecular and Cell Biology
11714603	7	Synthesis of antitumor dendritic imides.	University San Pablo-Ceu
11597418	47	Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.	Glaxosmithkline
32511913	141	Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.	Japan Tobacco
32676146	61	Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.	Biocon Bristol Myers Squibb Research Center
11277536	130	7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.	Novartis Pharma Research
32292564	138	Efficacy and Tolerability of Pyrazolo[1,5-	The Genomics Institute of The Novartis Research Foundation
32292555	44	Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.	University of Oxford
31830635	74	Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).	Peking University
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
11012022	102	Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.	Basf Bioresearch
11012021	69	Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.	Basf Bioresearch
27429068	54	Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.	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).	Bristol-Myers Squibb Research and Development
30755337	95	Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.	Japan Tobacco
31381333	302	Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.	TBA
30562697	84	The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.	University of Silesia In Katowice
10612598	29	4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.	Celltech Therapeutics
10476877	15	NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.	Abbott Laboratories
30986571	66	Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.	Zhejiang University
10377223	57	Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.	Merck Research Laboratories
30532965	81	Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.	Glaxosmithkline R&D
30300845	43	1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.	Universit£
10052978	22	Phosphotyrosine-containing dipeptides as high-affinity ligands for the p56lck SH2 domain.	Boehringer Ingelheim Pharmaceuticals
31693351	473	Discovery of 4	TBA
9873567	28	The development of novel and selective p56lck tyrosine kinase inhibitors.	R. W. Johnson Pharmaceutical Research Institute
31185168	144	Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.	Rti International
9871562	2	1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.	Bristol-Myers Squibb Pharmaceutical Research Institute
31244114	56	Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-? Motif Kinase (ZAK) Inhibitors.	Jinan University
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.	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).	Peking 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.	Sichuan University and Collaborative Innovation Center
9719597	12	Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.	Novartis Pharma
30878832	57	Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.	Arromax Pharmatech
9632358	45	Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design.	University of Arizona
9599224	10	Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.	Novartis Pharma
30529543	57	Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.	China Pharmaceutical University
30508668	62	Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation.	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.	University of Florida
31670517	41	Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.	West China Hospital of Sichuan University
31526603	379	Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.	Takeda Pharmaceutical
30807144	23	Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.	Cresset
31749904	74	Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.	Glaxosmithkline
31620238	50	Discovery of Pyridazinone and Pyrazolo[1,5-	Bristol-Myers Squibb
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.	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.	Abbvie Bioresearch Center
8474097	19	Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.	National Cancer Institute-Bethesda
8411019	6	Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors.	National Institutes of Health
8411012	19	Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.	Purdue University
8105084	6	Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors.	National Institutes of Health
8064792	25	5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.	Sterling Winthrop Pharmaceuticals Research Division
7932563	60	Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src.	Purdue University
7902440	104	Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.	Hebrew University of Jerusalem
23131412	30	Purpuroines A-J, halogenated alkaloids from the sponge Iotrochota purpurea with antibiotic activity and regulation of tyrosine kinases.	Peking University
10395524	3	A new tyrosine kinase inhibitor from the marine brown alga Stypopodium zonale.	Technical University of Braunschweig
10072676	15	Acquisition of high-affinity, SH2-targeted ligands via a spatially focused library.	The Albert Einstein College of Medicine of Yeshiva University
30380865	19	Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.	University of California San Diego
30249354	112	Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.	Glaxosmithkline R&D
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.	Sichuan University/Collaborative Innovation Center of Biotherapy
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.	Bristol-Myers Squibb
30082069	359	ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.	Vertex Pharmaceuticals
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals
29545102	159	Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.	Merck
30075624	71	Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.	Jinan University
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
29057049	53	Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.	Genomics Institute of The Novartis Research Foundation
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.	Sichuan University and Collaborative Innovation Center
28720503	146	Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.	Merck
1995903	49	Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues.	Purdue University
28259529	31	Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.	The Ohio State University
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.	Chinese Academy of Sciences
28945083	33	In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.	National Institute of Biological Sciences, Beijing
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
16135699	173	Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.	Acadia Pharmaceuticals
15590769	16	Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.	I.G.B.M.C.
11714898	21	Functional calcitonin gene-related peptide subtype 2 receptors in porcine coronary arteries are identified as calcitonin gene-related peptide subtype 1 receptors by radioligand binding and reverse transcription-polymerase chain reaction.	Creighton University
12616631	18	D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.	University of Queensland Brisbane
20028400	4	High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.	Nankai University
18849972	45	Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.	The Scripps Research Institute
11817957	58	Complexation and chiral recognition thermodynamics of 6-amino-6-deoxy-beta-cyclodextrin with anionic, cationic, and neutral chiral guests: counterbalance between van der Waals and coulombic interactions.	Japan Science and Technology Agency
15857113	12	Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.	Gsk
16190743	78	Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.	Merck Research Laboratories
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