The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
26800309 |
90 |
Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
Sygnature Discovery |
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 |
23442188 |
4 |
A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling. |
Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences |
23142618 |
66 |
Discovery of a novel series of 4-quinolone JNK inhibitors. |
Roche Palo Alto |
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 |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
18359226 |
50 |
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors. |
Bristol-Myers Squibb Research and Development |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
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 |
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 |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20637613 |
4 |
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3. |
Daiichi Sankyo |
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 |
20218619 |
44 |
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase. |
Amgen |
20148563 |
42 |
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. |
The Institute of Cancer Research |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
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 |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
18313298 |
40 |
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor. |
Bristol-Myers Squibb |
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 |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
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 |
30817889 |
11 |
Allosteric Modulator Discovery: From Serendipity to Structure-Based Design. |
Shanghai Jiao-Tong University School of Medicine |
31693351 |
473 |
Discovery of 4 |
TBA |
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 |
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 |
30978288 |
113 |
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
Northwestern University |
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 |
21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
9933142 |
67 |
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. |
Eli Lilly |