The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
27527804 |
109 |
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). |
Teva Branded Pharmaceutical Products R & D |
27144831 |
149 |
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
Ariad Pharmaceuticals |
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 |
27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
27106709 |
92 |
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening. |
Korea Research Institute of Chemical Technology |
26951750 |
59 |
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
26235945 |
58 |
Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor. |
Korea Research Institute of Chemical Technology |
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 |
25007344 |
73 |
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics. |
Christian-Albrechts-University of Kiel |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
25559205 |
31 |
Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor. |
Piramal Enterprises |
25180654 |
29 |
Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity. |
University of Paris |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
25271963 |
93 |
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
Astrazeneca |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
24900877 |
107 |
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors. |
Merck Research Laboratories |
24685542 |
67 |
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. |
Bristol-Myers Squibb Research and Development |
24900830 |
46 |
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
Vichem Chemie Research |
23906342 |
14 |
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. |
Takeda Pharmaceutical |
24157370 |
22 |
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. |
Chugai Pharmaceutical |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
24900590 |
55 |
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy. |
Glaxosmithkline |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23755884 |
23 |
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics. |
Takeda Pharmaceutical |
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 |
23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
23249297 |
75 |
Trimeric hemibastadin congener from the marine sponge Ianthella basta. |
Heinrich-Heine University |
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 |
23123015 |
22 |
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors. |
Takeda Pharmaceutical |
22883026 |
34 |
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives. |
Takeda Pharmaceutical |
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 |
22734674 |
81 |
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer. |
Amgen |
22141319 |
56 |
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors. |
Cephalon |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
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 |
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 |
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 |
24900237 |
41 |
Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity. |
TBA |
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 |
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 |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
21441024 |
74 |
Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors. |
Sanofi-Aventis |
21123062 |
48 |
Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors. |
Cephalon |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
20153646 |
28 |
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. |
Institute of Science and Technology |
20170163 |
157 |
Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation. |
Technische Universitat Braunschweig |
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 |
19716697 |
110 |
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II. |
Boehringer Ingelheim Pharmaceuticals |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
19610618 |
41 |
Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
University of South Florida |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
19522465 |
102 |
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
Boehringer Ingelheim Pharma |
19081716 |
57 |
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway. |
Glaxosmithkline |
9677190 |
49 |
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. |
University of California |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
18321716 |
7 |
ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds. |
Institute of Molecular Physiology |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
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 |
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 |
16480284 |
126 |
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. |
Pfizer |
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 |
22377675 |
44 |
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. |
Westf£Lische Wilhelms-Universit£T M£Nster |
22310227 |
89 |
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. |
Glaxosmithkline |
16476733 |
18 |
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity. |
University of Queensland |
22269278 |
50 |
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
Chugai Pharmaceutical |
22285571 |
49 |
QSAR studies for prediction of cross-ß sheet aggregate binding affinity and selectivity. |
The Ohio State University College of Medicine |
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 |
21967808 |
52 |
Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. |
Cephalon |
22169263 |
73 |
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases. |
Cephalon |
22154349 |
123 |
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
22101132 |
41 |
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
Shionogi |
22014550 |
337 |
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
Ansaris |
22061645 |
68 |
Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group. |
Cephalon |
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 |
21859094 |
61 |
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity. |
Cephalon |
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 |
21775140 |
69 |
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase. |
Astrazeneca |
21708465 |
141 |
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
St. Jude Children'S Research Hospital |
21632243 |
48 |
Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors. |
Cephalon |
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 |
21353551 |
23 |
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2. |
Osi Pharmaceuticals |
21414779 |
64 |
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. |
Amgen |
24900240 |
19 |
Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR. |
TBA |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
21074994 |
46 |
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models. |
Cephalon |
21190849 |
53 |
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines. |
Cephalon |
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 |
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 |
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 |
17376430 |
19 |
ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. |
The Hebrew University of Jerusalem |
20472447 |
45 |
Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK). |
Nycomed Pharma |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
20430619 |
73 |
8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors. |
Cephalon |
20397705 |
208 |
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
20382527 |
26 |
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. |
Bristol-Myers Squibb Research and Development |
20346655 |
117 |
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases. |
Abbott Laboratories |
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 |
19854052 |
420 |
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. |
Genomics Institute of The Novartis Research Foundation |
20178321 |
74 |
Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening. |
Chinese Academy of Sciences |
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 |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
19775160 |
79 |
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability. |
Takeda Pharmaceutical |
19362847 |
51 |
Design and synthesis of a novel tyrosine kinase inhibitor template. |
St. Jude Children'S Research Hospital |
1479375 |
215 |
Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor Agents |
TBA |
| 42 |
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation |
TBA |
19327989 |
40 |
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
Pfizer |
19317452 |
155 |
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4. |
Wyeth Research |
19246196 |
104 |
5-Aminomethylbenzimidazoles as potent ITK antagonists. |
Boehringer Ingelheim Pharmaceuticals |
19211246 |
320 |
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping. |
4Sc |
19101143 |
70 |
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). |
Glaxosmithkline |
19053831 |
39 |
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles. |
Institute of General Genetics |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
18819799 |
72 |
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk). |
Johnson & Johnson |
18819794 |
53 |
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead. |
Johnson & Johnson |
18793846 |
33 |
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. |
Genomics Institute of The Novartis Research Foundation |
18691885 |
60 |
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. |
Ariad Pharmaceuticals |
18529047 |
156 |
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. |
Eberhard-Karls University |
17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
18308565 |
70 |
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases. |
Cephalon |
18289854 |
44 |
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase. |
Bristol-Myers Squibb Research and Development |
17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
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 |
16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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 |
16198560 |
19 |
Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases. |
Imclone Systems |
16134929 |
22 |
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
Bristol-Myers Squibb |
15771417 |
48 |
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors. |
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 |
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 |
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 |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12039590 |
51 |
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Abbott Bioresearch Center |
32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
11000003 |
8 |
Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor. |
Merck Research Laboratories |
30755337 |
95 |
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. |
Japan Tobacco |
31493743 |
32 |
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors. |
Anadolu University |
30789735 |
61 |
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. |
The Institute of Cancer Research |
28528303 |
171 |
Discovery of a potent dual ALK and EGFR T790M inhibitor. |
Harvard Medical School |
31693351 |
473 |
Discovery of 4 |
TBA |
31419130 |
69 |
Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK). |
Zhejiang University |
29617135 |
16 |
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
Athenex |
30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
30188734 |
41 |
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. |
University of Arkansas For Medical Sciences |
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 |
9240345 |
33 |
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
Parke-Davis Pharmaceutical Research |
31804076 |
1 |
Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability. |
University of Utah |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
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 |
19271717 |
96 |
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium. |
Heinrich-Heine-Universitat |
18494522 |
244 |
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense. |
Heinrich-Heine-Universit£T |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
28988628 |
2 |
Challenges in the design of insulin and relaxin/insulin-like peptide mimetics. |
University of Melbourne |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29653895 |
210 |
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model. |
Glaxosmithkline |
28711351 |
74 |
Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
Rigel Pharmaceuticals |
2033582 |
2 |
Phosphonate-containing inhibitors of tyrosine-specific protein kinases. |
National Cancer Institute-Bethesda |
28438385 |
24 |
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth. |
Indiana University School of Medicine |
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 |
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 |
28385505 |
26 |
Novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety for anaplastic lymphoma kinase (ALK) inhibitor. |
University of Science & Technology |
27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
Aimst University |
25346162 |
16 |
Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors. |
Pontificia Universidad Catolica De Chile |
19743875 |
5 |
Characterization of the CHK1 allosteric inhibitor binding site. |
Pfizer |
21848665 |
9 |
Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands. |
Yeditepe University |
7681406 |
8 |
Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. |
Sanofi Recherche |
11567092 |
4 |
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors. |
Gsk |
16495061 |
8 |
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent. |
Johnson & Johnson Pharmaceutical |
16690314 |
13 |
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres. |
Merck Research Laboratories |
16916797 |
8 |
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics. |
Incyte |