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 |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
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 |
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 |
27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
26951750 |
59 |
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
26396685 |
19 |
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. |
Amgen |
26351728 |
96 |
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. |
Konkuk University |
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 |
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 |
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 |
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 |
25453808 |
101 |
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. |
Bristol-Myers Squibb |
25369270 |
93 |
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. |
Galapagos |
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 |
24461299 |
82 |
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. |
Fox Chase Chemical Diversity Center |
24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
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 |
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 |
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 |
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 |
10741557 |
26 |
Naphthyl ketones: a new class of Janus kinase 3 inhibitors. |
Astrazeneca |
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 |
23107482 |
82 |
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2. |
Genentech |
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 |
22698084 |
99 |
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. |
Genentech |
22591402 |
127 |
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors. |
Argenta Discovery |
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 |
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 |
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 |
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 |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
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 |
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 |
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 |
21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
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 |
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 |
21038853 |
133 |
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. |
Novartis Institutes For Biomedical Research |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
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 |
19762238 |
78 |
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). |
Cytopia Research |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
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 |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
12482439 |
51 |
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase. |
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 |
32479083 |
42 |
Identification of |
China Pharmaceutical University |
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 |
31831383 |
2 |
Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34. |
Brigham Young University |
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 |
27326341 |
142 |
Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors. |
Leo Pharma |
27578246 |
158 |
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors. |
Glaxosmithkline R&D |
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 |
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 |
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 |
31550151 |
17 |
The Exploration of Chirality for Improved Druggability within the Human Kinome. |
University of Arkansas For Medical Sciences |
30565923 |
34 |
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology. |
Eberhard Karls University T£Bingen |
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 |
31647655 |
114 |
Kinase Chemodiversity from the Arctic: The Breitfussins. |
Uit - The Arctic University of Norway |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
28626517 |
24 |
Janus-Associated Kinase 1 (JAK1) Inhibitors as Potential Treatment for Immune Disorders. |
Therachem Research Medilab (India) |
34271072 |
34 |
A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors. |
A*Star |
23578312 |
22 |
Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors. |
Nas of Ukraine |
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 |
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 |
22339993 |
8 |
Inhibition of bacterial virulence: drug-like molecules targeting the Salmonella enterica PhoP response regulator. |
Washington University |
11909603 |
1 |
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. |
Takeda Chemical Industries |
10604951 |
12 |
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization. |
University of Colorado |
9103528 |
17 |
PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties. |
Pharmacia & Upjohn |
12210991 |
24 |
Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. |
New York University |
6310078 |
55 |
Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, a new uptake inhibitor with selectivity for serotonin. |
Pfizer |
16492568 |
12 |
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design. |
Cyclacel |
17433696 |
19 |
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists. |
Astrazeneca |
19692239 |
23 |
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
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 |
19464171 |
87 |
Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma. |
Amgen |
19361197 |
54 |
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes. |
Universita Del Piemonte Orientale |
18954041 |
28 |
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP). |
University of Michigan |
18714982 |
44 |
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
Cephalon |
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 |
14521405 |
29 |
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. |
Bristol-Myers Squibb |
12946343 |
3 |
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors. |
Morphochem |
17114291 |
10 |
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression. |
Johns Hopkins 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 |
12061878 |
100 |
Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa. |
Aventis Pharma Deutschland |
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 |
16919457 |
144 |
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
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 |
16616489 |
29 |
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors. |
Institut Curie |
14552750 |
35 |
Identification of potent and novel small-molecule inhibitors of caspase-3. |
Sunesis Pharmaceuticals |
15012993 |
22 |
A new series of potent oxindole inhibitors of CDK2. |
Hoffmann-La Roche |
15916442 |
52 |
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles. |
Wyeth Research |
11728184 |
20 |
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity. |
Biocryst Pharmaceuticals |
11689083 |
41 |
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. |
Wyeth-Ayerst Research |
7520079 |
13 |
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
Merck Research Laboratories |