The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27187860 |
18 |
Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
Yonsei University |
27155464 |
35 |
Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
Rallis India |
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 |
27374241 |
2 |
A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant. |
Universit£ |
27115835 |
85 |
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
University of Edinburgh |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
27189674 |
84 |
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
Beni-Suef University |
27010810 |
24 |
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
Oribase Pharma |
26555154 |
36 |
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
University of Edinburgh |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
27011159 |
97 |
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
Experimental Therapeutics Centre |
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 |
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 |
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 |
26789553 |
10 |
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia. |
High Magnetic Field Laboratory |
26698536 |
56 |
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
Chinese Academy of Sciences |
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 |
26451772 |
42 |
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
First Affiliated Hospital of Xi'An Jiaotong University |
26526740 |
111 |
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
Univ. Lille |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26298495 |
20 |
Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib. |
Xi'An Jiaotong University |
26286460 |
25 |
Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration. |
University of Michigan |
26231079 |
26 |
Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents. |
Xi'An Jiaotong 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 |
26195136 |
32 |
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
Guangzhou Institutes of Biomedicine and Health |
26022079 |
15 |
Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors. |
Beijing University of Technology |
25469771 |
37 |
Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma. |
Universit£ |
25965804 |
80 |
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
Eli Lilly |
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 |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
25699576 |
42 |
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
University of South Florida |
25757603 |
79 |
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
Siedlce University of Natural Sciences and Humanities |
25022204 |
78 |
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. |
Universit£ |
24785465 |
80 |
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
Chinese Academy of Sciences |
25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
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 |
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 |
24681986 |
42 |
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
Siedlce University of Natural Sciences and Humanities |
24440479 |
4 |
Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III. |
Shandong University |
24417566 |
43 |
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
Icahn School of Medicine At Mount Sinai |
24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
24280068 |
4 |
Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level. |
The University of Texas M.D. Anderson Cancer Center |
24183742 |
40 |
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
Chinese Academy of Sciences |
24157370 |
22 |
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. |
Chugai Pharmaceutical |
23993328 |
41 |
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
Chinese Academy of Sciences |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
24036042 |
2 |
Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II. |
Shandong University |
23937569 |
22 |
Selectivity data: assessment, predictions, concordance, and implications. |
Eli Lilly |
23920481 |
25 |
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. |
The Institute of Cancer Research |
23900004 |
5 |
Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties. |
University of Padova |
23790540 |
17 |
Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL. |
Korea Advanced Institute of Science and Technology |
24015327 |
42 |
Development of a chimeric c-Src kinase and HDAC inhibitor. |
University of Michigan |
24900720 |
2 |
Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors. |
Universit£ |
23773153 |
33 |
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
Technical University of Dortmund |
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 |
23746084 |
25 |
Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant. |
Universit£ |
23611771 |
8 |
The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
Novartis Institutes For Biomedical Research |
23602444 |
2 |
Cyclic peptides containing tryptophan and arginine as Src kinase inhibitors. |
University of Rhode Island |
23538233 |
16 |
Design, synthesis and biological activities of Nilotinib derivates as antitumor agents. |
Xi'An Jiaotong University |
23474386 |
26 |
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors. |
Chinese Academy of Sciences |
23473682 |
69 |
BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives. |
The First People'S Hospital of Hangzhou |
23434140 |
35 |
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis. |
East China University of Science and Technology |
23301767 |
154 |
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities. |
University of Nottingham |
22749189 |
24 |
Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
Institut Curie |
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 |
23253074 |
38 |
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
University of Zurich |
23441572 |
55 |
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. |
Cyclofluidic |
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 |
23301703 |
20 |
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
Chinese Academy of Sciences |
23273517 |
53 |
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors. |
National Center For Advancing Translational Sciences |
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 |
23088644 |
39 |
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)¿isoleucine(315) mutant. |
Chinese Academy of Sciences |
24900387 |
11 |
Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics. |
TBA |
24900538 |
27 |
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. |
TBA |
22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
22853993 |
18 |
A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation. |
University of Siena |
22320388 |
116 |
Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity. |
University of Washington |
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 |
24900482 |
32 |
Targeted kinase selectivity from kinase profiling data. |
TBA |
22795629 |
59 |
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1. |
University of Washington |
22404346 |
52 |
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. |
The Institute of Cancer Research |
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 |
22369268 |
29 |
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1. |
University of Washington |
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 |
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 |
21116453 |
51 |
Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii. |
University of Washington |
15975507 |
13 |
Features of selective kinase inhibitors. |
University of California San Francisco |
20674368 |
12 |
New effective inhibitors of the Abelson kinase. |
Iowa State University |
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 |
20561787 |
46 |
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases. |
The Institute of Cancer Research |
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 |
20117004 |
68 |
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
University of Milano-Bicocca |
20038108 |
19 |
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance. |
Wyeth Research |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
19610618 |
41 |
Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
University of South Florida |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
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 |
17371799 |
12 |
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr |
Targegen |
17684099 |
4 |
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
Center For Molecular Medicine of The Austrian Academy of Sciences |
18324759 |
133 |
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors. |
Amgen |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
17983756 |
55 |
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. |
Osi Pharmaceuticals |
18257513 |
13 |
Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. |
Universit£ |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
17887663 |
34 |
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors. |
Pfizer |
17376680 |
18 |
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. |
Nippon Shinyaku |
17113292 |
73 |
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. |
Targegen |
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 |
16678414 |
25 |
3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors. |
Chiron |
16686543 |
44 |
Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. |
Universit£ |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
12477352 |
85 |
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
Novartis Pharma |
12238930 |
94 |
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. |
Kyowa Hakko Kogyo |
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 |
7608909 |
66 |
[(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase. |
Ciba |
1652014 |
44 |
Sulfonylbenzoyl-nitrostyrenes: potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase. |
Ciba-Geigy |
22221201 |
32 |
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
University of Kentucky |
22269278 |
50 |
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
Chugai Pharmaceutical |
22136433 |
67 |
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. |
Ludwig-Maximilians University of Munich |
22154349 |
123 |
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
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 |
22033461 |
4 |
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors. |
Beijing National Laboratory For Molecular Sciences |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
21958547 |
108 |
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
Pfizer |
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 |
21856155 |
45 |
Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells. |
University of Siena |
21823617 |
58 |
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
21812414 |
106 |
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
Pfizer |
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 |
21536449 |
16 |
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin. |
The Institute of Cancer Research |
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 |
21561771 |
39 |
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
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 |
21443205 |
33 |
Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study. |
University of Siena |
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 |
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 |
21322567 |
18 |
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
University of Strasburg |
21376587 |
15 |
Hybrid compounds as new Bcr/Abl inhibitors. |
Chinese Academy of Sciences |
21353551 |
23 |
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2. |
Osi Pharmaceuticals |
21341678 |
49 |
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. |
Millennium Pharmaceuticals |
24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
21080629 |
153 |
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity. |
University of Regensburg |
21035334 |
55 |
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. |
Martin-Luther-University Halle-Wittenberg |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
20961062 |
42 |
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity. |
Pfizer |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20828158 |
92 |
Expanding the diversity of allosteric bcr-abl inhibitors. |
Harvard Medical School |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
20817538 |
16 |
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
Novartis Institutes For Biomedical Research |
20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
20188579 |
42 |
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase. |
Temple University |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
19039322 |
50 |
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
Center For Molecular Medicine of The Austrian Academy of Sciences |
16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
16415863 |
2 |
Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
Genomics Institute of The Novartis Research Foundation |
16408016 |
6 |
Assignment of protein function in the postgenomic era. |
The Scripps Research Institute |
20655209 |
18 |
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. |
Université |
20604564 |
2 |
A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl. |
Harvard Medical School |
20513156 |
44 |
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
20409618 |
31 |
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold. |
Technische Universit£T Braunschweig |
20451394 |
10 |
Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms. |
Institute of Molecular Genetics Igm-Cnr |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
20462263 |
127 |
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. |
Cyclacel |
20218623 |
68 |
Emerging targets in osteoporosis disease modification. |
Amgen |
20397705 |
208 |
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
20363128 |
42 |
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors. |
Wyeth Research |
19894727 |
164 |
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. |
Wyeth Research |
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 |
20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
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 |
19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth Research |
20143778 |
70 |
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. |
Curis |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
19945869 |
7 |
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR. |
Taisho Pharmaceutical |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19889540 |
76 |
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. |
Memorial Sloan-Kettering Cancer Center |
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 |
19410338 |
44 |
Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data. |
Universit£ |
19572547 |
51 |
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. |
Ariad Pharmaceuticals |
| 230 |
Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives |
TBA |
| 47 |
The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands |
TBA |
| 31 |
Novel phosphotyrosine mimetics in the design of peptide ligands for pp60src SH2 domain |
TBA |
19356929 |
17 |
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
19301902 |
104 |
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
University of Regensburg |
19109024 |
5 |
Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases. |
Santen Pharmaceutical |
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 |
18691885 |
60 |
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. |
Ariad Pharmaceuticals |
18621522 |
18 |
N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds. |
Università |
18554909 |
50 |
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
Amgen |
18447379 |
96 |
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
Amgen |
18342402 |
77 |
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. |
Università |
18313174 |
26 |
Synthesis and biological evaluation of diversely substituted indolin-2-ones. |
Université |
17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
18248988 |
16 |
Entry into a new class of protein kinase inhibitors by pseudo ring design. |
Novartis Institutes For Biomedical Research |
17956080 |
4 |
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
Memorial Sloan-Kettering Cancer Center |
17827012 |
30 |
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes. |
Targegen |
17827009 |
116 |
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors. |
Tanabe Research Laboratories Usa |
17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
17572088 |
11 |
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties. |
Mcgill University/Royal Victoria Hospital |
17560108 |
5 |
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
Boehringer Ingelheim Pharmaceuticals |
17149885 |
20 |
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor. |
Eberhard-Karls University |
16970400 |
14 |
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
University of Milano-Bicocca |
16931012 |
61 |
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors. |
Targegen |
16722646 |
24 |
A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors. |
Università |
16722630 |
100 |
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. |
University of Regensburg |
16451066 |
58 |
Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase. |
Chembridge Research Laboratories and Chembridge |
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 |
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 |
15501042 |
18 |
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases. |
Novartis Institutes For Biomedical Research |
15177482 |
90 |
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. |
Novartis Institutes For Biomedical Research |
12951113 |
11 |
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase. |
Mcgill University/Royal Victoria Hospital |
11277536 |
130 |
7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src. |
Novartis Pharma Research |
11277535 |
80 |
7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src. |
Novartis Pharma Research |
10999468 |
30 |
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. |
Bayer Research Center |
10853665 |
104 |
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src. |
Novartis Pharma |
10090785 |
63 |
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. |
Novartis |
9784108 |
22 |
Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity. |
Warner-Lambert |
8691423 |
89 |
4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase. |
Ciba Pharmaceuticals |
8151612 |
88 |
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. |
Ciba-Geigy |
21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
21143042 |
30 |
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors. |
Shandong University |
28056160 |
3 |
Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library. |
X-Chem Pharmaceuticals |
27474804 |
19 |
Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies. |
Universiti Teknologi Mara (Uitm) |
27289559 |
38 |
Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids. |
Tehran University of Medical Sciences |
27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
Aimst University |
16690725 |
29 |
Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo. |
Eli Lilly |
16554355 |
47 |
N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors. |
University of Kansas |
16492761 |
51 |
An efficient rapid system for profiling the cellular activities of molecular libraries. |
Genomics Institute of The Novartis Research Foundation |
16436501 |
8 |
Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor. |
Meiji Seika Kaisha |
15764739 |
7 |
Desensitization of the human motilin receptor by motilides. |
Katholieke Universiteit Leuven |
18849971 |
56 |
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
University of California San Francisco |
17163639 |
13 |
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis. |
Suny Stony Brook |