The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27940419 |
31 |
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands. |
Comenius University In Bratislava |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
27994755 |
18 |
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization. |
Merck |
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 |
25625541 |
58 |
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors. |
Merck |
25043312 |
104 |
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides. |
University Health Network |
25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
24773549 |
20 |
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties. |
Development Center For Biotechnology |
23920481 |
25 |
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. |
The Institute of Cancer Research |
23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
22819505 |
46 |
Discovery and characterization of novel allosteric FAK inhibitors. |
Takeda Pharmaceutical |
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 |
24900658 |
10 |
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. |
Hoffmann-La Roche |
23312943 |
166 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
22995819 |
4 |
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine. |
TBA |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
23082860 |
69 |
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
The Institute of Cancer Research |
22746295 |
91 |
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach. |
Teijin Pharma |
22551018 |
68 |
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas. |
Astrazeneca |
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 |
22564207 |
44 |
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. |
Cephalon |
22404346 |
52 |
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. |
The Institute of Cancer Research |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
22148921 |
48 |
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c |
Cephalon |
21334796 |
4 |
Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of I¿B kinase-ß. |
Universidade Federal Do Rio De Janeiro |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
20561787 |
46 |
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases. |
The Institute of Cancer Research |
20022510 |
61 |
Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2. |
The Institute of Cancer Research |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
17360485 |
10 |
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. |
Millennium Pharmaceuticals |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
22285028 |
22 |
Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors. |
Michigan State University |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
22111927 |
65 |
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
The Institute of Cancer Research |
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 |
21794960 |
194 |
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
Universit£ |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21536449 |
16 |
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin. |
The Institute of Cancer Research |
21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
20630752 |
40 |
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors. |
Millennium Pharmaceuticals |
21186793 |
72 |
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. |
The Institute of Cancer Research |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20673630 |
38 |
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration. |
Astrazeneca R&D Boston |
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 |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19791746 |
14 |
Kinase inhibitor data modeling and de novo inhibitor design with fragment approaches. |
Eli Lilly |
17937984 |
46 |
2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2. |
Johnson & Johnson Pharmaceutical Research & Development |
17658776 |
109 |
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. |
Abbott Laboratories |
17287122 |
79 |
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. |
Abbott Laboratories |
17035018 |
25 |
Identification of novel, selective and potent Chk2 inhibitors. |
Valeant Pharmaceutical Research and Development 3300 Hyland Avenue |
16934458 |
124 |
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors. |
Valeant Pharmaceuticals Research & Development |
16442290 |
12 |
Novel non-benzimidazole chk2 kinase inhibitors. |
Johnson and Johnson Pharmaceutical Research and Development |
15771432 |
48 |
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. |
Johnson & Johnson Pharmaceutical Research and Development |
15261294 |
17 |
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. |
Michigan State University |
14640546 |
46 |
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin |
Cephalon |
10821800 |
61 |
Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. |
Friedrich-Schiller-University Jena |