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 |
| 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 |
| 27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
| 26762835 |
342 |
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2). |
Icahn School Of Medicine At Mount Sinai |
| 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 |
| 24938496 |
32 |
Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept. |
Aska Pharmaceutical |
| 25393557 |
83 |
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives. |
Translational Research Institute |
| 23498914 |
32 |
Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects. |
Hanyang University |
| 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 |
| 23416002 |
126 |
Amino acid derived quinazolines as Rock/PKA inhibitors. |
Translational Research Institute |
| 19303774 |
87 |
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3. |
Glaxosmithkline |
| 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 |
| 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 |
| 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 |
| 22905713 |
9 |
Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
Astellas Pharma |
| 22257213 |
98 |
Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
Rigel |
| 22746295 |
91 |
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach. |
Teijin Pharma |
| 23002419 |
30 |
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules. |
TBA |
| 22858099 |
52 |
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy. |
Korea University |
| 22320327 |
250 |
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series. |
Amgen |
| 19751974 |
81 |
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. |
Pfizer |
| 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 |
| 18578517 |
93 |
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
Eberhard Karls University Tuebingen |
| 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 |
| 18278858 |
93 |
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen |
| 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 |
| 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 |
| 15177483 |
33 |
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity. |
Novartis Institutes For Biomedical Research |
| 11844702 |
14 |
Pyridazine based inhibitors of p38 MAPK. |
Merck Research Laboratories |
| 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 |
| 21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21936542 |
143 |
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
Novartis Institute For Biomedical Research |
| 21813278 |
95 |
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration. |
Elan Pharmaceuticals |
| 20594847 |
62 |
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I. |
Novartis Institutes For Biomedical Research |
| 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 |
| 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 |
| 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 |
| 20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
| 20655210 |
3 |
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors. |
Roche Palo Alto |
| 20395140 |
42 |
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase. |
Pfizer |
| 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 |
| 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 |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 19928858 |
77 |
Displacement assay for the detection of stabilizers of inactive kinase conformations. |
Chemical Genomics Centre Of The Max Planck Society |
| 19591487 |
38 |
3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. |
Eberhard-Karls University |
| 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 |
| 19356929 |
17 |
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 19327989 |
40 |
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
Pfizer |
| 18817365 |
73 |
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold. |
Amgen |
| 18539026 |
5 |
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells. |
Cardiff University |
| 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 |
| 18207396 |
10 |
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors. |
Eberhard-Karls University |
| 17658737 |
2 |
Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
Boehringer Ingelheim Pharmaceuticals |
| 17570666 |
64 |
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
Pfizer |
| 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 |
| 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 |
| 17010605 |
2 |
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase. |
Boehringer Ingelheim Pharmaceuticals |
| 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 |
| 16249085 |
26 |
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity. |
Novartis Institutes For Biomedical Research |
| 15943486 |
8 |
Rapid computational identification of the targets of protein kinase inhibitors. |
University Of Iowa |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 15615541 |
2 |
Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase. |
Serono Pharmaceutical Research Institute |
| 15177482 |
90 |
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. |
Novartis Institutes For Biomedical Research |
| 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 |
| 12086485 |
10 |
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
Boehringer Ingelheim Pharmaceuticals |
| 11597418 |
47 |
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. |
Glaxosmithkline |
| 10866395 |
33 |
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors. |
Novartis Pharma |
| 10377223 |
57 |
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
Merck Research Laboratories |
| 9873604 |
72 |
Pyrroles and other heterocycles as inhibitors of p38 kinase. |
Merck Research Laboratory |
| 27996267 |
22 |
Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
University Of Pittsburgh |
| 21381887 |
3 |
Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers. |
Aristotle University Of Thessaloniki |
| 27616456 |
21 |
Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as a-glucosidase inhibitors. |
Jishou University |
| 9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
| 2905002 |
8 |
Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity. |
Schering-Plough |
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