405 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
28665128	86	Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.	Principia Biopharma
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
27996259	2	Spiro Meroterpenoids from Ganoderma applanatum.	Chinese Academy of Sciences
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
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
27839918	28	Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).	Takeda California
27771180	49	Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.	Central China Normal University
27994736	28	Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a	Dalian Medical 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
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
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
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
26396685	19	Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.	Amgen
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
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26288683	43	Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.	Bristol-Myers Squibb R & D
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang University
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
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
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
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
25369270	93	Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.	Galapagos
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
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
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
24650640	43	Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.	Martin-Luther-University Halle-Wittenberg
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
24359159	60	Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.	Astrazeneca
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
23937569	22	Selectivity data: assessment, predictions, concordance, and implications.	Eli Lilly
23867602	122	Lead identification of novel and selective TYK2 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
23562594	33	Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.	Astrazeneca
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
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
23312943	166	Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
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
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
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
22698084	99	Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.	Genentech
22591402	127	Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.	Argenta Discovery
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
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
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
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
21106455	60	Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.	Sri International
15975507	13	Features of selective kinase inhibitors.	University of California San Francisco
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
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
18359226	50	Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.	Bristol-Myers Squibb Research and Development
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	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.	Amgen
18083554	54	N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.	Amgen
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
16451062	46	Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.	Astrazeneca
22221201	32	VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.	University of Kentucky
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
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
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
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
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
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
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
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
24900229	41	Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.	TBA
21282055	30	Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.	Bristol-Myers Squibb
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
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research and Development
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
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
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
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
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
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
19414255	58	Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.	Vertex Pharmaceuticals
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
19019674	24	Fragment-based discovery of JAK-2 inhibitors.	Sgx Pharmaceuticals
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
18682324	33	Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.	Amgen
18667312	24	Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.	The Scripps Research Institute
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
17088059	25	Simplified staurosporine analogs as potent JAK3 inhibitors.	Johnson & Johnson Pharmaceutical Research and Development
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
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
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
16216497	67	Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.	Abbott Bioresearch Center
15566298	34	The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.	Bristol-Myers Squibb
15546730	9	Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
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
12941344	18	Mapping the kinase domain of Janus Kinase 3.	Aventis Pharmaceuticals
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
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
32122740	27	Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.	East China University of Science & Technology
32001089	8	Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.	University of Strathclyde
31980341	31	Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.	Takeda Pharmaceutical
32527540	51	Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.	Shenyang Pharmaceutical University
32253095	78	Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.	Pfizer
32479083	42	Identification of	China Pharmaceutical University
31866272	17	Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.	Dalian Medical University
32462873	216	Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.	Gvk Biosciences
31843459	57	Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.	Chia Tai Tianqing Pharmaceutical Group
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
30853331	95	Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.	China Pharmaceutical University
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
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
27326341	142	Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors.	Leo Pharma
31266686	7	Small-molecule agents for the treatment of inflammatory bowel disease.	Gilead Sciences
27774135	6	Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1	Shandong University
27555284	27	The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.	Gwangju Institute of Science and Technology (Gist)
27544589	52	Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3.	Astellas Pharma
31609613	244	Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.	TBA
31381333	302	Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.	TBA
30113844	240	Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).	Pfizer
32297743	59	Discovery of (2	Astrazeneca
32134643	66	Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.	Janssen Research and Development
30891145	70	Identification of Imidazo[1,2-	Bristol-Myers Squibb
30846405	102	Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.	China Pharmaceutical University
31417666	55	Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.	Vertex Pharmaceuticals
30532965	81	Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.	Glaxosmithkline R&D
31693351	473	Discovery of 4	TBA
31318208	123	Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.	TBA
32083858	145	Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.	TBA
31550151	17	The Exploration of Chirality for Improved Druggability within the Human Kinome.	University of Arkansas For Medical Sciences
30565923	34	Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.	Eberhard Karls University T£Bingen
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
30901208	96	Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.	Shandong 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
30878832	57	Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.	Arromax Pharmatech
30981578	46	Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.	East China University of Science & Technology
30926315	75	Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.	Central China Normal University
30987781	88	Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.	Southeast University
30891131	60	Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.	Bristol-Myers Squibb
30615446	69	Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.	Peking University
30530193	64	Targeting the immunity protein kinases for immuno-oncology.	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
31050421	48	Overview of Recent Strategic Advances in Medicinal Chemistry.	Shandong University
29870256	16	Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.	Genentech
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.	Pfizer
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
29969256	21	Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.	Universitaire Vaudois
30243158	80	Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.	National University of Singapore
30423248	226	Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.	Pfizer
30460842	111	Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.	Purdue University
29578342	35	Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.	Yunnan University
29247857	102	A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.	Beijing Normal University
29146136	32	Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.	The First Affiliated Hospital of Dalian Medical University
30145050	27	Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.	Astellas Pharma
30139575	98	Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.	China Pharmaceutical University
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
30006143	14	Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.	Dalian Medical University
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals
28615111	24	Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives.	Universit£
29452839	82	Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.	Seoul National University
28844493	14	Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.	Eberhard-Karls-University Tuebingen
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.	Advinus Therapeutics
29631132	33	The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.	Shaanxi University of Science & Technology
29940115	55	Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.	Second Military Medical University
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
29856615	85	Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.	Astrazeneca
28628824	98	Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.	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.	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.	Sichuan University and Collaborative Innovation Center
28539220	198	Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.	Bristol-Myers Squibb Research and Development
28259529	31	Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.	The Ohio State University
28947151	62	Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.	Bristol-Myers Squibb
28927786	52	Discovery of highly potent, selective, covalent inhibitors of JAK3.	Bristol-Myers Squibb Research and Development
28830649	101	Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.	Genentech
29156136	160	The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.	Merck
28953386	66	Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.	National University of Singapore
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.	University of Science and Technology of China
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
28626517	24	Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders.	Therachem Research Medilab (India)
28792760	35	Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.	Moffitt Cancer Center
28433531	69	Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.	Wuxi Apptec (Shanghai)
34271072	34	A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.	A*Star
23578312	22	Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.	Nas of Ukraine
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
11909603	1	T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.	Takeda Chemical Industries
11303063	11	Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.	Creighton University
10604951	12	Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.	University of Colorado
9832156	13	Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.	F. Hoffmann-La Roche
12210991	24	Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.	New York University
20028400	4	High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.	Nankai University
3272174	7	Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.	National Institute of Mental Health
16492568	12	Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.	Cyclacel
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
19361197	54	Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.	Universita Del Piemonte Orientale
19167883	5	Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.	Gilead Sciences
18042731	12	Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids.	The Johns Hopkins University
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
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
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
17201404	16	Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.	Glaxosmithkline
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
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
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
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