The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
| 27055065 |
92 |
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. |
The Institute Of Cancer 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 |
| 26704265 |
49 |
Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes. |
Semmelweis University |
| 26431428 |
36 |
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). |
Wuxi Apptec |
| 25261929 |
20 |
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies. |
Kakatiya University |
| 25893042 |
65 |
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors. |
Translational Research Institute |
| 25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£T T£Bingen |
| 25341110 |
66 |
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. |
Genentech |
| 25393557 |
83 |
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives. |
Translational Research Institute |
| 24650640 |
43 |
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors. |
Martin-Luther-University Halle-Wittenberg |
| 23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
| 23416002 |
126 |
Amino acid derived quinazolines as Rock/PKA inhibitors. |
Translational Research Institute |
| 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 |
| 15950471 |
20 |
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity. |
Astrazeneca |
| 24900510 |
16 |
Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. |
TBA |
| 19303774 |
87 |
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3. |
Glaxosmithkline |
| 17602798 |
54 |
3D-QSAR and docking studies of aminopyridine carboxamide inhibitors of c-Jun N-terminal kinase-1. |
Chinese Academy Of Sciences |
| 17194588 |
92 |
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. |
Glaxosmithkline |
| 22621397 |
39 |
Irreversible protein kinase inhibitors: balancing the benefits and risks. |
Covalution Pharma |
| 23147077 |
23 |
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. |
Takeda Pharmaceutical |
| 23142618 |
66 |
Discovery of a novel series of 4-quinolone JNK inhibitors. |
Roche Palo Alto |
| 23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
| 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 |
| 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 |
| 22257213 |
98 |
Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
Rigel |
| 24900545 |
21 |
Identification of an Adamantyl Azaquinolone JNK Selective Inhibitor. |
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 |
| 22858099 |
52 |
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy. |
Korea University |
| 22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
| 22564207 |
44 |
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. |
Cephalon |
| 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 |
| 22230199 |
12 |
Unbiased binding assays for discovering small-molecule probes and drugs. |
Broad Institute Of Harvard And Mit |
| 21353571 |
26 |
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells. |
Hanyang University |
| 19947601 |
24 |
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors. |
Translational Research Institute |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University Of Dundee |
| 19394223 |
50 |
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. |
Glaxosmithkline |
| 14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
| 18313930 |
30 |
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2). |
Takeda Pharmaceutical |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University Of Oxford |
| 18313304 |
50 |
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1). |
Takeda Pharmaceutical |
| 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 |
| 16451062 |
46 |
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. |
Astrazeneca |
| 15999997 |
85 |
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. |
Serono Pharmaceutical Research Institute |
| 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 |
| 22310227 |
89 |
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. |
Glaxosmithkline |
| 22244937 |
44 |
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. |
Celgene |
| 22226655 |
88 |
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury. |
Celgene |
| 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 |
| 22004719 |
56 |
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors. |
The Scripps Research Institute |
| 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 |
| 22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
| 21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21815634 |
11 |
Design and characterization of a potent and selective dual ATP- and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor. |
Sanford-Burnham Medical Research Institute |
| 21813278 |
95 |
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration. |
Elan Pharmaceuticals |
| 21699136 |
16 |
Selectivity of kinase inhibitor fragments. |
Glaxosmithkline |
| 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 |
| 21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
| 21570836 |
78 |
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement. |
Elan Pharmaceuticals |
| 21515047 |
24 |
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead. |
Roche Palo Alto |
| 21489792 |
26 |
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors. |
Korea Institute Of Science And Technology |
| 21458276 |
82 |
Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase. |
Sanford-Burnham Medical Research Institute |
| 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 |
| 21375264 |
77 |
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors |
Roche Palo Alto |
| 21316221 |
62 |
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors. |
The Scripps Research Institute |
| 24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
| 24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
| 21316234 |
133 |
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor. |
Elan Pharmaceuticals |
| 21112785 |
151 |
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration. |
Elan Pharmaceuticals |
| 21071223 |
190 |
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK. |
Elan Pharmaceuticals |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 20472330 |
16 |
Novel 8-arylated purines as inhibitors of glycogen synthase kinase. |
Institut Curie |
| 20146479 |
31 |
Small molecule JNK (c-Jun N-terminal kinase) inhibitors. |
Merck Research Laboratories |
| 19950901 |
23 |
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. |
Roche Palo Alto |
| 19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
| 19864136 |
45 |
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. |
Wyeth Research |
| 20060294 |
21 |
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy. |
Novartis Institutes For Biomedical Research |
| 20045647 |
35 |
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors. |
Institute For Medical Research |
| 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 |
| 19361991 |
80 |
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors. |
Vertex Pharmaceuticals |
| 19574047 |
42 |
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase. |
Amgen |
| 19327989 |
40 |
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
Pfizer |
| 19097792 |
24 |
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity. |
Astrazeneca R&D Boston |
| 18996009 |
36 |
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase. |
The Scripps Research Institute-Florida |
| 18817365 |
73 |
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold. |
Amgen |
| 18602262 |
56 |
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
Glaxosmithkline |
| 18494454 |
5 |
Development of paramagnetic probes for molecular recognition studies in protein kinases. |
Institute For Medical Research |
| 18482836 |
14 |
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding. |
Ucb Pharma |
| 17166835 |
12 |
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors. |
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti |
| 17459703 |
111 |
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
Ucb Pharma |
| 17289388 |
8 |
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors. |
Tibotec |
| 17055723 |
17 |
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases. |
Abbott Laboratories |
| 16971120 |
104 |
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond. |
Abbott Laboratories |
| 16970394 |
147 |
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen |
| 16516473 |
444 |
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors. |
Astrazeneca |
| 16337120 |
53 |
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3. |
Astrazeneca R&D SöDertäLje |
| 16162000 |
42 |
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. |
Takeda Pharmaceutical |
| 16140012 |
30 |
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3. |
Astrazeneca R&D SöDertäLje |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 15317461 |
53 |
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. |
Glaxosmithkline |
| 15177482 |
90 |
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. |
Novartis Institutes For Biomedical Research |
| 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 |
| 12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
| 12086491 |
116 |
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. |
Pharmaceutical Research Institute |
| 11597418 |
47 |
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. |
Glaxosmithkline |
| 10999468 |
30 |
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. |
Bayer Research Center |
| 10866395 |
33 |
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors. |
Novartis Pharma |
| 9873604 |
72 |
Pyrroles and other heterocycles as inhibitors of p38 kinase. |
Merck Research Laboratory |
| 27616456 |
21 |
Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as a-glucosidase inhibitors. |
Jishou University |
| 28340404 |
12 |
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives. |
Warsaw University Of Technology |
| 24133210 |
8 |
Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. |
Western University |
| 12683677 |
8 |
Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors. |
UniversitÉ |
| 8910290 |
5 |
Inactivation of a novel neuropeptide Y/peptide YY receptor gene in primate species. |
Yamanouchi Pharmaceutical |
| 2905001 |
64 |
McN-5652: a highly potent inhibitor of serotonin uptake. |
Mcneil Pharmaceutical |
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