The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28249207 |
78 |
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis. |
East China Normal University |
| 28692292 |
73 |
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers. |
Sichuan University and Collaborative Innovation Center For Biotherapy |
| 27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
| 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 |
| 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 |
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
| 27668758 |
17 |
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors. |
Kasetsart University |
| 27771180 |
49 |
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors. |
Central China Normal University |
| 27171036 |
164 |
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
University of Nebraska Medical Center |
| 27490956 |
59 |
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. |
Merck |
| 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 |
| 27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang 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 |
| 27137359 |
18 |
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. |
Shandong University |
| 27130359 |
55 |
Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors. |
China Pharmaceutical University |
| 26819674 |
66 |
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR. |
Genentech |
| 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 |
| 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 |
| 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 |
| 26384287 |
65 |
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors. |
Kangwon National University |
| 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 |
| 26344595 |
26 |
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
Xi'An Jiaotong University |
| 26277759 |
31 |
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors. |
China Pharmaceutical 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 |
| 26258521 |
104 |
Development of Selective Covalent Janus Kinase 3 Inhibitors. |
Harvard Medical School |
| 25662701 |
23 |
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents. |
Zhejiang University |
| 25262942 |
189 |
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping. |
Astrazeneca |
| 25262541 |
86 |
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines. |
Hoffmann-La Roche |
| 26059596 |
58 |
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors. |
Astellas Pharma |
| 26071372 |
89 |
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. |
Astellas Pharma |
| 25987372 |
104 |
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors. |
Bristol-Myers Squibb |
| 26121481 |
37 |
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿. |
Vertex Pharmaceuticals |
| 26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
| 25835317 |
63 |
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
Sichuan University |
| 25699576 |
42 |
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
University of South Florida |
| 25800646 |
40 |
Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2. |
Central South University |
| 25633741 |
67 |
Discovery and profiling of a selective and efficacious Syk inhibitor. |
Novartis Institutes For Biomedical Research |
| 25882525 |
26 |
Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders. |
Nerviano Medical Sciences |
| 25827523 |
275 |
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. |
Vertex Pharmaceuticals |
| 25650310 |
4 |
Computer-aided discovery of aminopyridines as novel JAK2 inhibitors. |
Chonnam National University |
| 25353650 |
111 |
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
Pfizer |
| 24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
| 24930833 |
136 |
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors. |
Syncom |
| 24913714 |
53 |
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres. |
Merck Research Laboratories |
| 25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
| 25453808 |
101 |
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. |
Bristol-Myers Squibb |
| 25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
| 25383627 |
85 |
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. |
Genentech |
| 25369270 |
93 |
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. |
Galapagos |
| 25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
| 24534486 |
56 |
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors. |
Novartis Institutes For Biomedical Research |
| 24417533 |
63 |
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. |
Pfizer |
| 24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
| 24779514 |
128 |
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. |
Gilead Sciences |
| 24726806 |
108 |
Syk inhibitors with high potency in presence of blood. |
Novartis Institutes For Biomedical Research |
| 24685542 |
67 |
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. |
Bristol-Myers Squibb Research and Development |
| 24666646 |
37 |
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms. |
Merck |
| 24582987 |
30 |
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization. |
Merck |
| 24569110 |
11 |
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk. |
University of Zurich |
| 24432909 |
13 |
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
Pfizer |
| 23810672 |
3 |
A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells. |
University of Toronto |
| 24461299 |
82 |
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. |
Fox Chase Chemical Diversity Center |
| 24389511 |
25 |
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. |
Zhejiang University |
| 24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
| 23993776 |
17 |
Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics. |
University of Zurich |
| 24398382 |
3 |
Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group. |
Konkuk University |
| 24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
| 24042009 |
89 |
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors. |
Genentech |
| 23867602 |
122 |
Lead identification of novel and selective TYK2 inhibitors. |
Genentech |
| 23870430 |
55 |
2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors. |
Genentech |
| 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 |
| 23642482 |
62 |
Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1. |
Argenta Discovery |
| 23668484 |
15 |
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. |
Genentech |
| 23659214 |
138 |
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2. |
Genentech |
| 23602398 |
43 |
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. |
Merck Research Laboratories |
| 23587425 |
37 |
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors. |
Merck Research Laboratories |
| 23562594 |
33 |
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target. |
Astrazeneca |
| 23535330 |
83 |
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. |
Merck Research Laboratories |
| 23541670 |
63 |
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors. |
Hoffmann-La Roche |
| 23540648 |
103 |
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome. |
F. Hoffmann-La Roche |
| 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 |
| 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 |
| 21903390 |
79 |
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
Glaxosmithkline |
| 23127890 |
96 |
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. |
Exelixis |
| 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 |
| 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 |
| 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 |
| 22591441 |
29 |
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling. |
Genentech |
| 22257213 |
98 |
Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
Rigel |
| 22698084 |
99 |
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. |
Genentech |
| 22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
| 24900538 |
27 |
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. |
TBA |
| 22591402 |
127 |
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors. |
Argenta Discovery |
| 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 |
| 22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
| 22594690 |
80 |
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. |
Cephalon |
| 22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
| 22542012 |
155 |
The design, synthesis, and biological evaluation of PIM kinase inhibitors. |
Exelixis |
| 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 |
| 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 |
| 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 |
| 22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
| 24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
| 22342147 |
55 |
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors. |
Astrazeneca R&D Boston |
| 21608528 |
166 |
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. |
Merck Research Laboratories |
| 21155605 |
39 |
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. |
Novartis Institutes For Biomedical Research |
| 21138246 |
44 |
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. |
Astrazeneca R&D |
| 21128646 |
88 |
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure. |
Merck Research Laboratories |
| 21106455 |
60 |
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. |
Sri International |
| 20138514 |
93 |
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
Vertex Pharmaceuticals |
| 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 |
| 19857967 |
103 |
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2. |
Vertex Pharmaceuticals |
| 19648005 |
41 |
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells. |
Amgen |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
| 19320489 |
125 |
Discovery and development of aurora kinase inhibitors as anticancer agents. |
Vertex Pharmaceuticals |
| 14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
| 18029174 |
10 |
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
Merck Frosst Centre For Therapeutic Research |
| 17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
| 17189692 |
32 |
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3). |
Procter and Gamble Pharmaceuticals |
| 16934457 |
60 |
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3. |
Procter and Gamble Pharmaceuticals |
| 16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
| 22148278 |
132 |
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase |
S Bio |
| 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 |
| 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 |
| 22119465 |
18 |
Structure-based design of PDK1 inhibitors. |
S Bio |
| 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 |
| 22041060 |
33 |
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation. |
Cephalon |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21970471 |
66 |
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia. |
Vertex Pharmaceuticals |
| 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 |
| 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 |
| 20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
| 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 |
| 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 |
| 24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
| 21288717 |
131 |
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions. |
Abbott Laboratories |
| 21282055 |
30 |
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3. |
Bristol-Myers Squibb |
| 21282054 |
178 |
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions. |
Abbott Laboratories |
| 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 |
| 21044843 |
29 |
The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead. |
Merck |
| 20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
| 20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
| 20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
| 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 |
| 20655209 |
18 |
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. |
Université |
| 20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
| 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 |
| 20172718 |
3 |
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing. |
Novartis Institutes For Biomedical Research |
| 20144546 |
11 |
Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors. |
Astrazeneca R&D Boston |
| 20138510 |
60 |
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors. |
Novartis Institutes For Biomedical Research |
| 19836234 |
46 |
2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors. |
Ligand Pharmaceuticals |
| 19762238 |
78 |
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). |
Cytopia Research |
| 19945871 |
62 |
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors. |
Vertex Pharmaceuticals |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 19857966 |
62 |
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors. |
Astrazeneca R&D Boston |
| 20014869 |
10 |
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. |
Vertex Pharmaceuticals |
| 19362847 |
51 |
Design and synthesis of a novel tyrosine kinase inhibitor template. |
St. Jude Children'S Research Hospital |
| 19447617 |
1 |
Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening. |
Semmelweis University |
| 19414255 |
58 |
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. |
Vertex Pharmaceuticals |
| 19097792 |
24 |
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity. |
Astrazeneca R&D Boston |
| 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 |
| 19019674 |
24 |
Fragment-based discovery of JAK-2 inhibitors. |
Sgx Pharmaceuticals |
| 18986805 |
39 |
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. |
Astrazeneca Pharmaceuticals |
| 18682324 |
33 |
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors. |
Amgen |
| 17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
| 17178722 |
1 |
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. |
University of Oklahoma Health Sciences Center |
| 18248988 |
16 |
Entry into a new class of protein kinase inhibitors by pseudo ring design. |
Novartis Institutes For Biomedical Research |
| 17350837 |
59 |
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors. |
Amgen |
| 17280833 |
52 |
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR. |
Amgen |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 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 |
| 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 |
| 32511913 |
141 |
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders. |
Japan Tobacco |
| 32122740 |
27 |
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors. |
East China University of Science & Technology |
| 32001089 |
8 |
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs. |
University of Strathclyde |
| 31980341 |
31 |
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors. |
Takeda Pharmaceutical |
| 32527540 |
51 |
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors. |
Shenyang Pharmaceutical University |
| 32253095 |
78 |
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1. |
Pfizer |
| 32435361 |
1 |
Chimeric Peptidomimetics of SOCS 3 Able to Interact with JAK2 as Anti-inflammatory Compounds. |
University of Naples "Federico Ii |
| 32462873 |
216 |
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity. |
Gvk Biosciences |
| 31843459 |
57 |
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
Chia Tai Tianqing Pharmaceutical Group |
| 32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
| 32292557 |
119 |
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases. |
Gilead Sciences |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 30853331 |
95 |
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors. |
China Pharmaceutical University |
| 30833158 |
51 |
The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors. |
Hungarian Academy of Sciences |
| 27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
| 27429068 |
54 |
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
Glaxosmithkline R&D |
| 27326341 |
142 |
Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors. |
Leo Pharma |
| 27774135 |
6 |
Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1 |
Shandong University |
| 27555284 |
27 |
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3. |
Gwangju Institute of Science and Technology (Gist) |
| 27544589 |
52 |
Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3. |
Astellas Pharma |
| 27531604 |
55 |
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177). |
Bristol-Myers Squibb Research and Development |
| 27519462 |
1 |
Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. |
Virginia Tech |
| 31609613 |
244 |
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases. |
TBA |
| 31314518 |
356 |
Identification of |
TBA |
| 30113844 |
240 |
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). |
Pfizer |
| 32297743 |
59 |
Discovery of (2 |
Astrazeneca |
| 32134643 |
66 |
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease. |
Janssen Research and Development |
| 30891145 |
70 |
Identification of Imidazo[1,2- |
Bristol-Myers Squibb |
| 30846405 |
102 |
Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold. |
China Pharmaceutical University |
| 31417666 |
55 |
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. |
Vertex Pharmaceuticals |
| 30532965 |
81 |
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach. |
Glaxosmithkline R&D |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 31318208 |
123 |
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. |
TBA |
| 31408808 |
12 |
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3. |
Shenyang Pharmaceutical University |
| 31207462 |
42 |
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital |
| 32329617 |
36 |
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core. |
Yale University |
| 31550151 |
17 |
The Exploration of Chirality for Improved Druggability within the Human Kinome. |
University of Arkansas For Medical Sciences |
| 31074988 |
95 |
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor. |
Vertex Pharmaceuticals (Europe) |
| 30565923 |
34 |
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology. |
Eberhard Karls University T£Bingen |
| 31077998 |
81 |
Targeting tropomyosin receptor kinase for cancer therapy. |
China Pharmaceutical University |
| 30927566 |
52 |
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
Shenyang Pharmaceutical University |
| 30901208 |
96 |
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. |
Shandong University |
| 30878832 |
57 |
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
Arromax Pharmatech |
| 30981578 |
46 |
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
East China University of Science & Technology |
| 30926315 |
75 |
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors. |
Central China Normal University |
| 30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
| 30891131 |
60 |
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis. |
Bristol-Myers Squibb |
| 30530193 |
64 |
Targeting the immunity protein kinases for immuno-oncology. |
China Pharmaceutical University |
| 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 |
| 31670517 |
41 |
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms. |
West China Hospital of Sichuan University |
| 31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
| 31050421 |
48 |
Overview of Recent Strategic Advances in Medicinal Chemistry. |
Shandong University |
| 29870256 |
16 |
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances. |
Genentech |
| 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 |
| 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 |
| 25009002 |
47 |
Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors. |
Nerviano Medical Sciences |
| 23275831 |
121 |
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). |
Moffitt Cancer Center |
| 31200237 |
95 |
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
Shanghai Pharmaceuticals Holding |
| 29969256 |
21 |
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. |
Universitaire Vaudois |
| 30249354 |
112 |
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. |
Glaxosmithkline R&D |
| 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 |
| 30170943 |
35 |
Design and synthesis of potent RSK inhibitors. |
Novartis Institutes For Biomedical Research |
| 30423248 |
226 |
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. |
Pfizer |
| 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 |
| 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 |
| 30097367 |
96 |
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series. |
Bristol-Myers Squibb |
| 30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
| 29945795 |
32 |
Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
National University of Singapore |
| 29545103 |
27 |
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90). |
National University of Singapore |
| 29545102 |
159 |
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor. |
Merck |
| 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 |
| 28844493 |
14 |
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting. |
Eberhard-Karls-University Tuebingen |
| 28279528 |
53 |
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis. |
Advinus Therapeutics |
| 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 |
| 28734581 |
37 |
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
Sichuan University and Collaborative Innovation Center |
| 28539220 |
198 |
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors. |
Bristol-Myers Squibb Research and Development |
| 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 |
| 28195723 |
94 |
Drug Discovery Targeting Bromodomain-Containing Protein 4. |
University of Texas Medical Branch |
| 27726390 |
41 |
Natural-Based Indirubins Display Potent Cytotoxicity toward Wild-Type and T315I-Resistant Leukemia Cell Lines. |
Beckman Research Institute |
| 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 |
| 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 |
| 28626521 |
4 |
Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders. |
Yale University |
| 28626520 |
8 |
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules. |
Yale University |
| 28626517 |
24 |
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders. |
Therachem Research Medilab (India) |
| 28478927 |
46 |
Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors. |
Martin-Luther-University Halle-Wittenberg |
| 28792760 |
35 |
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
Moffitt Cancer Center |
| 27791347 |
41 |
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. |
Pfizer |
| 27840070 |
28 |
Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. |
Eberhard Karls University Tuebingen |
| 25382253 |
6 |
Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1. |
University of Copenhagen |
| 16492761 |
51 |
An efficient rapid system for profiling the cellular activities of molecular libraries. |
Genomics Institute of The Novartis Research Foundation |
| 21439476 |
12 |
Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors. |
University of Luxembourg |
| 10467133 |
4 |
Structural basis for selective inhibition of Src family kinases by PP1. |
Princeton University |
| 16884310 |
97 |
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. |
Amgen |
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