The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
| 27644332 |
59 |
Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
Curtin University |
| 26854431 |
47 |
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines. |
La Trobe University |
| 26121481 |
37 |
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿. |
Vertex Pharmaceuticals |
| 26102506 |
40 |
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
Celgene |
| 25387153 |
53 |
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. |
University Hospital Hradec Kralove |
| 24893124 |
4 |
Development of synthetic lethality anticancer therapeutics. |
The University of Texas M.D. Anderson Cancer Center |
| 25589928 |
37 |
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors. |
Novartis Institutes For Biomedical Research |
| 25589927 |
36 |
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors. |
Novartis Institutes For Biomedical Research |
| 25589915 |
41 |
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
Monash University (Parkville Campus) |
| 24387221 |
150 |
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. |
Sanofi |
| 23855836 |
147 |
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. |
Newcastle University |
| 23726034 |
117 |
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. |
Novartis Institutes For Biomedical Research |
| 23662903 |
34 |
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. |
Genentech |
| 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 |
| 23394205 |
106 |
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
Astrazeneca |
| 23059543 |
39 |
Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
La Trobe University |
| 22835870 |
29 |
Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family. |
Astrazeneca |
| 22548365 |
293 |
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases. |
Amgen |
| 22863202 |
94 |
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. |
Novartis Institutes For Biomedical Research |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
| 12672248 |
50 |
Kinase inhibitors: not just for kinases anymore. |
Northwestern University |
| 21612232 |
113 |
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives. |
Amgen |
| 21664823 |
15 |
Synthesis, structural elucidation, DNA-PK inhibition, homology modelling and anti-platelet activity of morpholino-substituted-1,3-naphth-oxazines. |
La Trobe University |
| 21636270 |
27 |
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. |
Genentech |
| 21332118 |
157 |
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors. |
Amgen |
| 21413798 |
174 |
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. |
Vertex Pharmaceuticals |
| 21322566 |
61 |
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. |
Dana-Farber Cancer Institute |
| 21216595 |
38 |
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain. |
Newcastle University |
| 20860370 |
83 |
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. |
Dana-Farber Cancer Institute |
| 20822905 |
28 |
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase. |
Genentech |
| 20472428 |
27 |
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors. |
Newcastle University |
| 19762236 |
9 |
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase. |
Kudos Pharmaceuticals |
| 18678488 |
49 |
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK). |
Newcastle University |
| 17562705 |
6 |
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. |
Stony Brook University |
| 17371003 |
128 |
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase. |
Newcastle University |
| 16302822 |
116 |
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. |
School of Natural Sciences--Chemistry |
| 15658870 |
104 |
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. |
Newcastle University |
| 15546735 |
25 |
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. |
University of Newcastle |
| 12941339 |
23 |
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK). |
University of Newcastle |
| 11597411 |
4 |
Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035). |
Newcastle University |
| 11294389 |
27 |
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. |
Department of Molecular Oncogenesis |
| 32502336 |
79 |
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. |
Bayer |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 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 |
| 27259031 |
191 |
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase. |
Astrazeneca |
| 31851518 |
61 |
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- |
Astrazeneca |
| 31955578 |
37 |
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders. |
Novartis Institutes For Biomedical Research |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 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) |
| 30582813 |
67 |
Evolution of PI3K? and ? Inhibitors for Inflammatory and Autoimmune Diseases. |
Astrazeneca |
| 29211480 |
64 |
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy. |
China Pharmaceutical University |
| 26996374 |
75 |
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
| 26565666 |
82 |
Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). |
Cleave Biosciences |
| 30346772 |
124 |
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
Astrazeneca |
| 30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
| 30128072 |
68 |
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. |
Astrazeneca |
| 29683659 |
127 |
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one). |
Astrazeneca |
| 28947947 |
112 |
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. |
Novartis Institutes For Biomedical Research |
| 29847724 |
25 |
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase? (PI3K?) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS). |
Vertex Pharmaceuticals |
| 28838830 |
21 |
Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation. |
La Trobe University |
| 29308895 |
24 |
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer. |
Nankai University |
| 28829592 |
109 |
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
University of Basel |
| 23173744 |
18 |
Kinetic and in silico analysis of thiazolidin-based inhibitors of a-carbonic anhydrase isoenzymes. |
Ondokuz Mayis University |
| 12815170 |
15 |
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding. |
Abbott Laboratories |
| 19700331 |
76 |
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists. |
Ono Pharmaceutical |
| 19010686 |
58 |
Structure-activity relationship studies of 5-benzylaminoimidazo[1,2-c]pyrimidine-8-carboxamide derivatives as potent, highly selective ZAP-70 kinase inhibitors. |
Kissei Pharmaceutical |
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