277 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28249207	78	Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.	East China Normal University
28692292	73	Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.	Sichuan University And Collaborative Innovation Center For Biotherapy
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
27983835	81	Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.	Pfizer
27541357	58	Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.	National University Of Singapore
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University Of Sydney
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27668758	17	Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.	Kasetsart University
27771180	49	Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.	Central China Normal University
27171036	164	Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.	University Of Nebraska Medical Center
27490956	59	Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.	Merck
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27261178	32	Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.	Konkuk University
27089211	38	Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.	Zhejiang University
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
27137359	18	Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.	Shandong University
27130359	55	Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.	China Pharmaceutical University
26819674	66	Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.	Genentech
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
26927423	58	Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.	Merck
26701356	100	Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.	Takeda Pharmaceutical
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
26614408	106	Identification of azabenzimidazoles as potent JAK1 selective inhibitors.	Astrazeneca
26384287	65	Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.	Kangwon National University
26351728	96	Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.	Konkuk 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
26288683	43	Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.	Bristol-Myers Squibb R & D
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
26086931	38	Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.	Shandong University
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.	Xi'An Jiaotong University
26277759	31	Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.	China Pharmaceutical University
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
26258521	104	Development of Selective Covalent Janus Kinase 3 Inhibitors.	Harvard Medical School
25662701	23	Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.	Zhejiang University
25262942	189	Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.	Astrazeneca
25262541	86	Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.	Hoffmann-La Roche
26059596	58	Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.	Astellas Pharma
26071372	89	Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.	Astellas Pharma
25987372	104	9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.	Bristol-Myers Squibb
26121481	37	Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.	Vertex Pharmaceuticals
26005534	158	(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.	Genomics Institute Of The Novartis Research Foundation
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.	Sichuan University
25699576	42	Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.	University Of South Florida
25800646	40	Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.	Central South University
25633741	67	Discovery and profiling of a selective and efficacious Syk inhibitor.	Novartis Institutes For Biomedical Research
25882525	26	Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.	Nerviano Medical Sciences
25827523	275	Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.	Vertex Pharmaceuticals
25650310	4	Computer-aided discovery of aminopyridines as novel JAK2 inhibitors.	Chonnam National University
25353650	111	Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.	Pfizer
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24930833	136	Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.	Syncom
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
25453808	101	Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.	Bristol-Myers Squibb
25409491	83	A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.	Zhejiang University
25383627	85	Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.	Genentech
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
24534486	56	2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.	Novartis Institutes For Biomedical Research
24417533	63	Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.	Pfizer
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24779514	128	Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.	Gilead Sciences
24726806	108	Syk inhibitors with high potency in presence of blood.	Novartis Institutes For Biomedical Research
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research And Development
24666646	37	Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.	Merck
24582987	30	The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.	Merck
24569110	11	Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.	University Of Zurich
24432909	13	Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.	Pfizer
23810672	3	A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.	University Of Toronto
24461299	82	Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.	Fox Chase Chemical Diversity Center
24389511	25	Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.	Zhejiang University
24359159	60	Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.	Astrazeneca
23993776	17	Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.	University Of Zurich
24398382	3	Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.	Konkuk University
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24042009	89	Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.	Genentech
23867602	122	Lead identification of novel and selective TYK2 inhibitors.	Genentech
23870430	55	2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.	Genentech
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	Genomics Institute Of The Novartis Research Foundation
23642482	62	Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.	Argenta Discovery
23668484	15	Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.	Genentech
23659214	138	Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.	Genentech
23602398	43	Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.	Merck Research Laboratories
23587425	37	Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.	Merck Research Laboratories
23562594	33	Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.	Astrazeneca
23535330	83	Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.	Merck Research Laboratories
23541670	63	Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.	Hoffmann-La Roche
23540648	103	Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.	F. Hoffmann-La Roche
23394126	170	Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).	Exelixis
23265875	78	Design and synthesis of tricyclic cores for kinase inhibition.	Abbott Bioresearch Center
23214979	74	3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.	F. Hoffmann-La Roche
21903390	79	Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.	Glaxosmithkline
23127890	96	SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.	Exelixis
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
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
21604762	152	Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph	S*Bio
23116168	42	Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.	Sichuan University
23061660	92	Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.	Genentech
22591441	29	Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.	Genentech
22257213	98	Discovery and development of spleen tyrosine kinase (SYK) inhibitors.	Rigel
22698084	99	Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.	Genentech
22548342	210	Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.	Exelixis
24900538	27	Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.	TBA
22591402	127	Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.	Argenta Discovery
22795331	51	Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.	Janssen Pharmaceutical Companies Of Johnson & Johnson
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
22594690	80	A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.	Cephalon
22738630	76	Structure-based optimization of aminopyridines as PKC¿ inhibitors.	Vertex Pharmaceuticals
22542012	155	The design, synthesis, and biological evaluation of PIM kinase inhibitors.	Exelixis
22372864	25	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.	Hanmi Research Center
22339472	148	Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth	S Bio
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
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
22342147	55	Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.	Astrazeneca R&D Boston
21608528	166	Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.	Merck Research Laboratories
21155605	39	Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.	Novartis Institutes For Biomedical Research
21138246	44	Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.	Astrazeneca R&D
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
21106455	60	Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.	Sri International
20138514	93	3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.	Vertex Pharmaceuticals
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
19857967	103	2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.	Vertex Pharmaceuticals
19648005	41	Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.	Amgen
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
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
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University Of Oxford
18029174	10	Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.	Merck Frosst Centre For Therapeutic Research
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17189692	32	Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).	Procter And Gamble Pharmaceuticals
16934457	60	Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.	Procter And Gamble Pharmaceuticals
16249345	25	Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.	Glaxosmithkline
22148278	132	Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase	S Bio
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
22087750	145	Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.	Amgen
22169263	73	Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.	Cephalon
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
22119465	18	Structure-based design of PDK1 inhibitors.	S Bio
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
22041060	33	2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.	Cephalon
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21970471	66	Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.	Vertex Pharmaceuticals
21942426	113	Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.	Merck
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
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21561767	48	Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.	Ariad Pharmaceuticals
21493067	22	In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.	Astrazeneca R&D Boston
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
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
21288717	131	Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.	Abbott Laboratories
21282055	30	Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.	Bristol-Myers Squibb
21282054	178	Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.	Abbott Laboratories
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21105711	79	Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.	Pfizer
21044843	29	The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.	Merck
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
20655209	18	Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.	Université
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute Of Biomedical Research
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
20231096	81	Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.	Novartis Institutes For Biomedical Research
20172718	3	Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.	Novartis Institutes For Biomedical Research
20144546	11	Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.	Astrazeneca R&D Boston
20138510	60	2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.	Novartis Institutes For Biomedical Research
19836234	46	2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.	Ligand Pharmaceuticals
19762238	78	Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).	Cytopia Research
19945871	62	A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.	Vertex Pharmaceuticals
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19857966	62	Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.	Astrazeneca R&D Boston
20014869	10	Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.	Vertex Pharmaceuticals
19362847	51	Design and synthesis of a novel tyrosine kinase inhibitor template.	St. Jude Children'S Research Hospital
19447617	1	Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening.	Semmelweis University
19414255	58	Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.	Vertex Pharmaceuticals
19097792	24	Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.	Astrazeneca R&D Boston
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
19035792	85	Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.	Glaxosmithkline
19019674	24	Fragment-based discovery of JAK-2 inhibitors.	Sgx Pharmaceuticals
18986805	39	Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.	Astrazeneca Pharmaceuticals
18682324	33	Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.	Amgen
17185414	30	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.	Genomics Institute Of The Novartis Research Foundation
17178722	1	Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.	University Of Oklahoma Health Sciences Center
18248988	16	Entry into a new class of protein kinase inhibitors by pseudo ring design.	Novartis Institutes For Biomedical Research
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen
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
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
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
12482439	51	Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.	Merck Research Laboratories
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
29298069	206	Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.	Pfizer
28626521	4	Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.	Yale University
28626520	8	JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.	Yale University
28626517	24	Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.	Therachem Research Medilab (India)
28478927	46	Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.	Martin-Luther-University Halle-Wittenberg
28792760	35	Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.	Moffitt Cancer Center
22299575	2	Inhibition of acetylpolyamine and spermine oxidases by the polyamine analogue chlorhexidine.	University Roma Tre
22233543	70	New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.	Centre De Recherche De Gif
24644281	3	Fatty acid-binding protein 5 (FABP5) regulates cognitive function both by decreasing anandamide levels and by activating the nuclear receptor peroxisome proliferator-activated receptor ß/d (PPARß/d) in the brain.	Case Western Reserve University School Of Medicine
28181373	14	Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry.	Griffith University
28126289	11	Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors.	Panjab University
23884422	10	Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation.	Mcgill University
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
23363077	2	Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A.	University Of Kentucky
15590769	16	Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.	I.G.B.M.C.
19758807	23	Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts.	Universitat De Barcelona
19692239	23	Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.	Boehringer Ingelheim Pharmaceuticals
19179081	32	Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.	Yale University
18243697	77	Identification of a potent new chemotype for the selective inhibition of PDE4.	Nih
19464171	87	Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.	Amgen
19338356	21	Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.	Acadia Pharmaceuticals
19361197	54	Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.	Universita Del Piemonte Orientale
18954041	28	Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).	University Of Michigan
18714982	44	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.	Cephalon
18341273	16	Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.	Astrazeneca
16242339	63	Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.	Lund University
12946343	3	The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.	Morphochem
17114291	10	Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.	Johns Hopkins University
17636946	94	Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.	Gsk
11520194	13	Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).	University Of Illinois At Chicago
11731301	192	Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.	Axys Pharmaceutical
16434195	23	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16982190	46	Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.	Glaxosmithkline
16220987	133	Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.	Pfizer
16913695	12	Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).	Istituto Di Cristallografia
16919457	144	Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.	Merck Research Laboratories
12773032	4	3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.	University Of Bologna
14552750	35	Identification of potent and novel small-molecule inhibitors of caspase-3.	Sunesis Pharmaceuticals
15012993	22	A new series of potent oxindole inhibitors of CDK2.	Hoffmann-La Roche
11266159	63	3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).	Smithkline Beecham Pharmaceuticals
11689083	41	Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.	Wyeth-Ayerst Research
7520079	13	Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.	Merck Research Laboratories
9171880	21	Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors.	Dupont Pharmaceuticals