The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27983835 |
81 |
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin. |
Pfizer Inc |
| 27541357 |
58 |
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
National University of Singapore |
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck & Co. |
| 27490956 |
59 |
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. |
Merck KGaA |
| 27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
| 27261178 |
32 |
Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability. |
Konkuk University |
| 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 |
| 26927423 |
58 |
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors. |
Merck & Co. |
| 26701356 |
100 |
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors. |
Takeda Pharmaceutical Co., Ltd |
| 26632965 |
80 |
Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents. |
Duke University School of Medicine |
| 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 |
| 26614408 |
106 |
Identification of azabenzimidazoles as potent JAK1 selective inhibitors. |
AstraZeneca |
| 26351728 |
96 |
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. |
Konkuk University |
| 26320619 |
88 |
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 26288683 |
43 |
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. |
Bristol-Myers Squibb R & D |
| 26288682 |
64 |
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors. |
Bristol-Myers Squibb Research & Development |
| 26086931 |
38 |
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators. |
Shandong University |
| 26231159 |
1 |
Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design. |
Chungnam National 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 srl |
| 26258521 |
104 |
Development of Selective Covalent Janus Kinase 3 Inhibitors. |
Harvard Medical School |
| 25987372 |
104 |
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors. |
Bristol-Myers Squibb Co. |
| 25699576 |
42 |
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
University of South Florida |
| 25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£t T£bingen |
| 24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
| 25453808 |
101 |
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. |
Bristol-Myers Squibb Co. |
| 25383627 |
85 |
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. |
Genentech Inc |
| 25369270 |
93 |
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. |
Galapagos NV |
| 24417533 |
63 |
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. |
Pfizer Inc |
| 24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
| 24042009 |
89 |
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors. |
Genentech Inc |
| 23265875 |
78 |
Design and synthesis of tricyclic cores for kinase inhibition. |
Abbott Bioresearch Center |
| 23214979 |
74 |
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. |
F. Hoffmann-La Roche Inc |
| 23127890 |
96 |
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. |
Exelixis Inc |
| 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 Ltd |
| 21604762 |
152 |
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph |
S*BIO Pte Ltd |
| 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 |
| 23061660 |
92 |
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. |
Genentech |
| 22698084 |
99 |
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. |
Genentech |
| 21413800 |
56 |
A one-pot synthesis and biological activity of ageladine A and analogues. |
Macquarie University |
| 22591402 |
127 |
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors. |
Argenta Discovery Ltd |
| 22339472 |
148 |
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth |
S BIO Pte. Ltd |
| 21155605 |
39 |
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. |
Novartis Institutes for BioMedical Research |
| 21106455 |
60 |
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. |
SRI International |
| 19648005 |
41 |
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells. |
Amgen Inc |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 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 Inc |
| 17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
| 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 |
| 22087750 |
145 |
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors. |
Amgen Inc |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21942426 |
113 |
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders. |
Merck & Co. |
| 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 |
| 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 srl |
| 24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
| 21105711 |
79 |
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. |
Pfizer Inc |
| 21035336 |
42 |
5-amino-pyrazoles as potent and selective p38a inhibitors. |
Bristol-Myers Squibb Research and Development |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 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 |
| 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 |
| 20138510 |
60 |
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors. |
Novartis Institutes for BioMedical Research |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 19053756 |
27 |
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). |
National Human Genome Research Institute |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
GlaxoSmithKline |
| 17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of the Novartis Research Foundation |
| 16970394 |
147 |
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen Inc |
| 16216497 |
67 |
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. |
Abbott Bioresearch Center |
| 12482439 |
51 |
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase. |
Merck Research Laboratories |
| 11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
| 28139931 |
85 |
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. |
Pfizer Inc. |
| 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 |
| 30243158 |
80 |
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. |
National University of Singapore |
| 30423248 |
226 |
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. |
Pfizer Inc. |
| 30460842 |
111 |
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
Purdue University |
| 30145050 |
27 |
Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor. |
Astellas Pharma Inc. |
| 30139575 |
98 |
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors. |
China Pharmaceutical University |
| 29452839 |
82 |
Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor. |
Seoul National University |
| 29293000 |
22 |
Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. |
University of Sharjah |
| 29631132 |
33 |
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
Shaanxi University of Science & Technology |
| 29940115 |
55 |
Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
Second Military Medical University |
| 29856615 |
85 |
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors. |
AstraZeneca |
| 29852068 |
86 |
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold. |
Eberhard Karls University T£bingen |
| 28539220 |
198 |
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors. |
Bristol-Myers Squibb Research and Development |
| 28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
| 28927786 |
52 |
Discovery of highly potent, selective, covalent inhibitors of JAK3. |
Bristol-Myers Squibb Research and Development |
| 28830649 |
101 |
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model. |
Genentech |
| 29156136 |
160 |
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties. |
Merck & Co. Inc |
| 28953386 |
66 |
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
National University of Singapore |
| 29298069 |
206 |
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. |
Pfizer Inc |
| 22233543 |
70 |
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis. |
Centre de Recherche de Gif |
| 20939767 |
13 |
Synthesis and SAR comparative studies of 2-allyl-4-methoxy-1-alkoxybenzenes as 15-lipoxygenase inhibitors. |
Mashhad University of Medical Sciences |
| 28181373 |
14 |
Characterisation of Photoaffinity-Based Chemical Probes by Fluorescence Imaging and Native-State Mass Spectrometry. |
Griffith University |
| 28126289 |
11 |
Synthesis, biological evaluation and in silico studies of 5-(3-methoxybenzylidene)thiazolidine-2,4-dione analogues as PTP1B inhibitors. |
Panjab University |
| 27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
AIMST University |
| 11909603 |
1 |
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. |
Takeda Chemical Industries, Ltd |
| 12210991 |
24 |
Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. |
New York University |
| 16492568 |
12 |
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design. |
Cyclacel Ltd |
| 19758807 |
23 |
Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts. |
Universitat de Barcelona |
| 19179081 |
32 |
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents. |
Yale University |
| 18243697 |
77 |
Identification of a potent new chemotype for the selective inhibition of PDE4. |
NIH |
| 19361197 |
54 |
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes. |
Universita del Piemonte Orientale |
| 18341273 |
16 |
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design. |
AstraZeneca |
| 16242339 |
63 |
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors. |
Lund University |
| 11520194 |
13 |
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase). |
University of Illinois at Chicago |
| 11731301 |
192 |
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets. |
Axys Pharmaceutical |
| 17201404 |
16 |
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity. |
GlaxoSmithKline |
| 16434195 |
23 |
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 16982190 |
46 |
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs. |
GlaxoSmithKline |
| 16913695 |
12 |
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819). |
Istituto di Cristallografia |
| 12773032 |
4 |
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy. |
University of Bologna |
| 14552750 |
35 |
Identification of potent and novel small-molecule inhibitors of caspase-3. |
Sunesis Pharmaceuticals |
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