The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
27362616 |
41 |
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives. |
Universit£ |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast 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 |
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 |
26233434 |
115 |
Design, synthesis and biological characterization of selective LIMK inhibitors. |
Amakem Therapeutics |
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 |
26039570 |
100 |
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors. |
Vertex Pharmaceuticals |
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 |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
25462247 |
20 |
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor. |
Fudan University |
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 |
22320327 |
250 |
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series. |
Amgen |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
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 |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University of Dundee |
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 |
16460940 |
13 |
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. |
Hoffmann-La Roche |
16451062 |
46 |
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. |
Astrazeneca |
12672248 |
50 |
Kinase inhibitors: not just for kinases anymore. |
Northwestern University |
12166950 |
208 |
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
Millennium Pharmaceuticals |
10843211 |
38 |
Structure-activity relationship studies of flavopiridol analogues. |
Mitotix |
9990463 |
69 |
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors. |
Novartis Pharmaceuticals |
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 |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
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 |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
20397705 |
208 |
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
19800227 |
31 |
Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases. |
University of Tartu |
19632115 |
105 |
4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors. |
Vertex Pharmaceuticals |
| 42 |
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation |
TBA |
| 230 |
Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives |
TBA |
| 77 |
Synthesis and protein kinase C inhibitory activities of indane analogs of balanol |
TBA |
| 90 |
Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors |
TBA |
| 23 |
Selective inhibition of the tyrosine kinase pp60src by analogs of 5,10-dihydropyrimido[4,5-b]quinolin-4(1H)-one |
TBA |
17716894 |
4 |
Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases. |
University of Tartu |
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 |
17125267 |
4 |
Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases. |
Institute of Organic and Bioorganic Chemistry |
16765046 |
63 |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
Chiron |
16686533 |
89 |
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies. |
Boehringer Ingelheim Pharmaceuticals |
16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16610779 |
10 |
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. |
Università |
16516473 |
444 |
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors. |
Astrazeneca |
16366598 |
51 |
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. |
Johnson & Johnson Pharmaceutical Research and Development |
16216497 |
67 |
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. |
Abbott Bioresearch Center |
15566298 |
34 |
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. |
Bristol-Myers Squibb |
14552791 |
35 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
Eli Lilly |
12941331 |
96 |
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
12941313 |
20 |
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. |
Novartis Pharma |
12824047 |
99 |
Novel IKK inhibitors: beta-carbolines. |
Millennium Pharmaceuticals |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12036347 |
116 |
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. |
Aventis Pharma Deutschland |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
30755337 |
95 |
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. |
Japan Tobacco |
30594029 |
42 |
CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors. |
Shaoxing University |
31417666 |
55 |
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. |
Vertex Pharmaceuticals |
9873567 |
28 |
The development of novel and selective p56lck tyrosine kinase inhibitors. |
R. W. Johnson Pharmaceutical Research Institute |
30384048 |
365 |
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
University of Florida |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
9003521 |
249 |
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety. |
Eli Lilly |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
28506751 |
4 |
Recent progress towards clinically relevant ATP-competitive Akt inhibitors. |
Merck |
22957720 |
5 |
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors. |
Ankara University |
22686946 |
12 |
Cytotoxic and potent CYP1 inhibitors from the marine algae Cymopolia barbata. |
University of The West Indies |
15302680 |
1 |
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892. |
Abbott Laboratories |
1968985 |
56 |
Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents. |
Niigata College of Pharmacy |
| 120 |
SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C. |
Sphinx Laboratories |