214 articles for thisTarget

---

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

PMID	Data	Article Title	Organization
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
28541695	192	Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).	East China University Of Science And Technology
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
27750146	58	Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.	Chinese Academy Of Sciences
28523108	113	2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.	Chinese Academy Of Sciences
27914362	54	An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.	The First Affiliated Hospital Of Zhengzhou University
28190652	26	Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
27829519	18	Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer.	Wenzhou Medical Universtiy
27884697	65	3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization.	Cxs
27933954	122	Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.	Chugai Pharmaceutical
27299736	37	The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.	St. John'S University
27348537	60	Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.	East China University Of Science & Technology
27131066	36	An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.	Chinese Academy Of Sciences
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast 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
27117427	77	Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors.	Chinese Academy Of Sciences (Cas)
27106711	87	Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).	Green Valley Research Institute
27017541	25	Design, synthesis and biological evaluation of 5-amino-4-(1H-benzoimidazol-2-yl)-phenyl-1,2-dihydro-pyrrol-3-ones as inhibitors of protein kinase FGFR1.	Nas Of Ukraine
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
26698536	56	Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.	Chinese Academy Of Sciences
26753815	81	Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.	The First Affiliated Hospital Of Xi'An Jiaotong University
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
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
22983304	4	Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.	Bristol-Myers Squibb
21289073	8	Metabolism and disposition of [14C]brivanib alaninate after oral administration to rats, monkeys, and humans.	Bristol-Myers Squibb
25699576	42	Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.	University Of South Florida
25827399	52	Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.	Chinese Academy Of Sciences
25791677	15	Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.	Zhengzhou University
25474320	10	Nintedanib: from discovery to the clinic.	Boehringer Ingelheim Pharma
25817240	33	Design, synthesis and biological evaluation of N-phenylthieno[2,3-d]pyrimidin-4-amines as inhibitors of FGFR1.	Institute Of Molecular Biology And Genetics Nas Of Ukraine
25736993	65	Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs.	Health Science Center Xi'An Jiaotong University
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
25589926	20	Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.	Astex Pharmaceuticals
25467150	5	Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3ß (GSK-3ß) with cellular activity of promoting glucose uptake.	Fudan University
25440884	2	Synthetic derivatives of aromatic abietane diterpenoids and their biological activities.	Universidad De Valencia
24801610	52	Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.	Universit£
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24904961	27	Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.	Qilu Pharmaceutical
24900886	66	Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.	Chinese Academy Of Sciences
24773549	20	Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.	Development Center For Biotechnology
24565969	69	Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.	Chinese Academy Of Sciences
24359159	60	Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.	Astrazeneca
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
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
24900658	10	Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.	Hoffmann-La Roche
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
22765894	223	The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.	Exelixis
22612866	123	Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.	Astrazeneca
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
23123015	22	Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.	Takeda Pharmaceutical
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
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
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
22863529	31	Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.	Chinese Academy Of Sciences
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
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
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
22148921	48	Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c	Cephalon
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
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20570525	56	Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.	Chinese Academy Of Sciences
20420387	118	Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.	Glaxosmithkline
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
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
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
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
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
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
16876403	85	Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.	Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
16460940	13	Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.	Hoffmann-La Roche
16451062	46	Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.	Astrazeneca
12477352	85	Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.	Novartis Pharma
12166950	208	Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.	Millennium Pharmaceuticals
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
22070629	61	Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).	Millennium Pharmaceuticals
22169262	26	Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.	Shenyang Pharmaceutical University
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
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
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
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
21665484	37	Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.	Chinese Academy Of Sciences
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
20630752	40	Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.	Millennium Pharmaceuticals
21561767	48	Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.	Ariad Pharmaceuticals
21517068	45	Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.	East China University Of Science And Technology
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
21405128	47	Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.	Chinese Academy Of Sciences
21441027	96	Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.	Astrazeneca
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
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
20833551	54	N-phenyl-N'-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases.	Takeda Pharmaceutical
20833055	44	Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.	Takeda Pharmaceutical
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
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
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
20188552	75	Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).	Wyeth Research
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
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
20121196	12	Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.	Yale University
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott 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
19877644	6	Identification of death-associated protein kinases inhibitors using structure-based virtual screening.	Pharmadesign
	42	A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation	TBA
	22	1-Oxo-3-aryl-1H-indene-2-carboxylic acid derivatives as selective inhibitors of fibroblast growth factor receptor-1 tyrosine kinase	TBA
19113866	129	Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.	Novartis Institutes For Biomedical Research
19110422	12	5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.	Mahidol University
19097792	24	Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.	Astrazeneca R&D Boston
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
18986805	39	Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.	Astrazeneca Pharmaceuticals
18610999	24	Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.	Institute Of Materia Medica
17185414	30	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.	Genomics Institute Of The Novartis Research Foundation
9139660	4	Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.	New York University Medical Center
18248988	16	Entry into a new class of protein kinase inhibitors by pseudo ring design.	Novartis Institutes For Biomedical Research
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
17658776	109	Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.	Abbott Laboratories
17618113	6	Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.	Mahidol University
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
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
16750628	47	Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.	Abbott Laboratories
16603352	89	Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.	Chiron
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
16446087	76	Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.	Chiron
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
16321529	30	Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.	Korea Research Institute Of Chemical Technology
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
14684325	154	Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.	Sugen
14640546	46	A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin	Cephalon
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
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
29016121	44	Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.	Novartis Institutes For Biomedical Research
28411455	45	Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization.	Shanghai Pharmaceuticals Holding
28714692	232	Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.	University Of Chinese Academy Of Sciences
28433531	69	Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.	Wuxi Apptec (Shanghai)
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
25298094	28	Plant-derived flavones as inhibitors of aurora B kinase and their quantitative structure-activity relationships.	Konkuk University
15999145	62	Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.	Case Western Reserve University
19549076	26	Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes.	Universita Degli Studi Di Firenze
1321043	17	Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.	UniversitÉ
10980448	3	Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.	Pfizer
10322128	13	Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.	Ligand Pharmaceuticals
21079602	5	Ultrasensitive in situ visualization of active glucocerebrosidase molecules.	Leiden University
	48	Thermodynamic and Nuclear Magnetic Resonance Study of the Reactions of α- and β-Cyclodextrin with Acids, Aliphatic Amines, and Cyclic Alcohols	Nist
19836248	35	3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.	Wyeth Research
17638903	6	Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.	University Hospital Basel
19167883	5	Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.	Gilead Sciences
19012392	15	Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases.	Shanghai Institute Of Organic Chemistry
17463090	3	Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.	University Of Central Florida College Of Medicine
16509577	52	Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.	Gsk
16632353	14	Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.	Abbott Laboratories
17168540	20	Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.	Genentech
14971907	180	Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.	Universita Degli Studi Di Firenze
16289938	24	Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.	Vernalis (R&D)
16945533	33	p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design.	Merck Research Laboratories
16759861	76	Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.	Pfizer
9822558	25	(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.	Schering-Plough Research Institute
16699172	59	Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.	German Cancer Research Center
11292354	48	A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.	Axys Pharmaceuticals
16916797	8	Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.	Incyte
17110106	78	Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.	Abbott Laboratories
12767917	30	Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.	St. Mary'S Hospital
10479289	55	Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.	Rhone-Poulenc Rorer
17181177	4	Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.	University Of Michigan
17034148	51	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.	Abbott Laboratories
15771423	98	Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.	University Of Antwerp
16978863	42	3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.	Merck Research Laboratories
16870442	18	Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.	Hawaii Biotech
16913712	21	Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening.	Montana State University
24059701	21	Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.	Qingdao University
15908206	164	Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.	Merck Research Laboratories
16759095	56	Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.	Abbott Laboratories
16722663	12	Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.	Universita Di Siena
11063609	36	Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.	Bristol-Myers Squibb Pharmaceutical Research Institute