The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28131714 |
119 |
Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß. |
Novartis Institutes For Biomedical Research |
28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
1597853 |
2 |
A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1. |
National Cancer Institute-Frederick |
1992155 |
30 |
Design of potent protein kinase inhibitors using the bisubstrate approach. |
Ura Cnrs 1309 |
2342075 |
11 |
Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties. |
University of North Carolina |
11454465 |
4 |
Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication. |
Glaxosmithkline |
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 |
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 |
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 |
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 |
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 |
25808573 |
3 |
Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships. |
National Cancer Institute-Bethesda |
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 |
25633741 |
67 |
Discovery and profiling of a selective and efficacious Syk inhibitor. |
Novartis Institutes For Biomedical Research |
25766633 |
9 |
Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor. |
The University of Michigan Medical School |
25437619 |
88 |
Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones). |
Seoul National University |
25000588 |
72 |
Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. |
Abbvie Bioresearch Center |
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 |
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 |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
25254961 |
32 |
Optimized protein kinase C¿ (PKC¿) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis. |
Abbvie Bioresearch Center |
24794745 |
20 |
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP. |
National Institute of Industrial Technology |
23434140 |
35 |
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis. |
East China University of Science and Technology |
23301767 |
154 |
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities. |
University of Nottingham |
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 |
23398373 |
88 |
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases. |
Vertex Pharmaceuticals |
23265875 |
78 |
Design and synthesis of tricyclic cores for kinase inhibition. |
Abbott Bioresearch Center |
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 |
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 |
23039927 |
44 |
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases. |
Martin-Luther-University Halle-Wittenberg |
21797275 |
139 |
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis. |
Novartis Institutes For Biomedical Research |
22078216 |
146 |
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes. |
Novartis Institutes For Biomedical Research |
22625994 |
28 |
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity. |
Kyoto University |
22533818 |
84 |
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a. |
Technische Universit£T Darmstadt |
22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
22537682 |
6 |
Inverse Virtual Screening allows the discovery of the biological activity of natural compounds. |
Universit£ |
21435888 |
7 |
The synthesis and evaluation of indolylureas as PKCa inhibitors. |
Procter & Gamble Pharmaceuticals |
21141896 |
2 |
Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase. |
P. Angeletti S.P.A. (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 |
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 |
20138512 |
82 |
Discovery of potent and bioavailable GSK-3beta inhibitors. |
Roche Palo Alto |
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 |
20038108 |
19 |
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance. |
Wyeth Research |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
9677190 |
49 |
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. |
University of California |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
9834166 |
8 |
Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity. |
Virginia Polytechnic Institute and State University |
18395443 |
37 |
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor. |
Bristol-Myers Squibb |
18359226 |
50 |
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors. |
Bristol-Myers Squibb Research and Development |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
17983756 |
55 |
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. |
Osi Pharmaceuticals |
17977729 |
40 |
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
Kyoto University |
17339109 |
33 |
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. |
Astellas Pharma |
17284021 |
10 |
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups. |
National Cancer Institute-Frederick |
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 |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
15999997 |
85 |
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. |
Serono Pharmaceutical Research Institute |
15380221 |
58 |
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. |
Central Pharmaceutical Research Institute |
14736244 |
8 |
Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones. |
National Cancer Institute-Frederick |
12672248 |
50 |
Kinase inhibitors: not just for kinases anymore. |
Northwestern University |
12954055 |
47 |
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. |
Johnson and Johnson Pharmaceutical Research and Development |
12801241 |
4 |
Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain. |
National Cancer Institute-Frederick |
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 |
8691452 |
1 |
Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C. |
National Cancer Institute-Bethesda |
8289196 |
7 |
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C. |
University of North Carolina |
10999477 |
40 |
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
Kyoto University |
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 |
| 80 |
Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure |
TBA |
16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
15953730 |
13 |
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation. |
Hoffmann-La Roche |
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 |
22204902 |
9 |
Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases. |
Institute of The Sir Mortimer Jewish General Hospital |
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 |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
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 |
21823617 |
58 |
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
21807510 |
31 |
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas. |
Technische Universit£T Darmstadt |
21880495 |
5 |
Chemical modifications of resveratrol for improved protein kinase C alpha activity. |
University of Houston |
21705217 |
60 |
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors. |
Bristol-Myers Squibb |
21696964 |
12 |
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP. |
Keio University |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
21548579 |
4 |
Hippolides A-H, acyclic manoalide derivatives from the marine sponge Hippospongia lachne. |
Second Military Medical University |
21596562 |
9 |
Design and synthesis of protein kinase Ca activators based on 'out of pocket' interactions. |
Riken Advanced Science Institute |
21561771 |
39 |
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
21035336 |
42 |
5-amino-pyrazoles as potent and selective p38a inhibitors. |
Bristol-Myers Squibb Research and Development |
20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20817520 |
40 |
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity. |
Kyoto University |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
10998351 |
24 |
Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
University of Dundee |
20684591 |
87 |
Identification of orally available naphthyridine protein kinase D inhibitors. |
Novartis Institutes For Biomedical Research |
20382527 |
26 |
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. |
Bristol-Myers Squibb Research and Development |
19894727 |
164 |
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. |
Wyeth Research |
20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
20188552 |
75 |
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
19864136 |
45 |
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. |
Wyeth Research |
19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth Research |
20045644 |
32 |
Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents. |
Seoul National University |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
19945867 |
39 |
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR. |
Taisho Pharmaceutical |
19888761 |
52 |
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer. |
Hanmi Research Center |
8882431 |
4 |
Antineoplastic agents. 340. Isolation and structural elucidation of bryostatins 16-18. |
Arizona State University |
| 4 |
Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II |
TBA |
| 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 |
| 70 |
Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety |
TBA |
| 90 |
Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors |
TBA |
| 8 |
Protein kinase C-α inhibitors; structure-activity relationships in bis-indole series |
TBA |
| 40 |
Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol |
TBA |
| 88 |
Novel PKC inhibitory analogs of balanol with replacement of the ester functionality |
TBA |
| 40 |
Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements |
TBA |
| 2 |
Synthesis of the benzofuran analogue of ILV, a new protein kinase C (PKC) activator |
TBA |
| 7 |
Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of α-alkylidene-γ-lactones with protein kinase C (PK-C) |
TBA |
| 4 |
Synthesis of ingenol analogs wth affinity for protein kinase C |
TBA |
| 3 |
Conformationally constrained analogues of diacylglycerol. 5. 2,5-Dideoxy-3-O-tetradecanoyl-D-galactono-1,4-lactone: A superior homologue of 3-O-tetradecanoyl-2-deoxy-L-ribonolactone with PK-C binding affinity. |
TBA |
19438240 |
8 |
Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C. |
University of Helsinki |
19379015 |
40 |
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths. |
National Cancer Institute-Frederick |
19364658 |
113 |
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
Wyeth Research |
19285393 |
90 |
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors. |
Glaxosmithkline |
19109017 |
4 |
(-)-Cercosporamide derivatives as novel antihyperglycemic agents. |
Daiichi Sankyo |
19081248 |
12 |
Identification of small molecules that inhibit GSK-3beta through virtual screening. |
Korea Research Institute of Chemical Technology |
18707088 |
72 |
Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins. |
National Cancer Institute-Frederick |
18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
17848581 |
13 |
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. |
Wyeth Research |
17395590 |
2 |
Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII. |
University of Wisconsin |
18072722 |
42 |
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
Kyoto University |
17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
16789733 |
41 |
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16765046 |
63 |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
Chiron |
16722637 |
39 |
Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions. |
National Cancer Institute-Frederick |
16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16640328 |
13 |
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta. |
Kyoto University |
16570908 |
39 |
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. |
Pharmaceutical Research Institute |
16539391 |
21 |
Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators. |
Research Institute of Pharmaceutical Sciences |
16216497 |
67 |
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. |
Abbott Bioresearch Center |
16134942 |
19 |
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C. |
National Cancer Institute-Frederick |
15943473 |
136 |
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15771419 |
134 |
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
Johnson & Johnson Pharmaceutical Research & Development |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
15615512 |
21 |
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15566298 |
34 |
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. |
Bristol-Myers Squibb |
15317463 |
16 |
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15261294 |
17 |
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. |
Michigan State University |
15163204 |
18 |
Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands. |
National Cancer Institute At Frederick |
15149684 |
59 |
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
15125969 |
8 |
Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C. |
Tohoku University |
14552791 |
35 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
Eli Lilly |
12954072 |
46 |
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity. |
Georgetown University Medical Center |
12941331 |
96 |
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
12941324 |
66 |
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes. |
Kyoto University |
12824047 |
99 |
Novel IKK inhibitors: beta-carbolines. |
Millennium Pharmaceuticals |
12749884 |
126 |
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. |
Eli Lilly |
12699375 |
10 |
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C). |
National Cancer Institute-Frederick |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12540236 |
11 |
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. |
Georgetown University Medical Center |
12270156 |
8 |
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a. |
Cephalon |
12039590 |
51 |
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Abbott Bioresearch Center |
11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
11909733 |
30 |
Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
Institute of Molecular and Cell Biology |
11728178 |
15 |
Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity. |
Seoul National University |
11689073 |
4 |
Iridals are a novel class of ligands for phorbol ester receptors with modest selectivity for the RasGRP receptor subfamily. |
University of Michigan Cancer Center |
11597418 |
47 |
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. |
Glaxosmithkline |
11327599 |
25 |
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth. |
Georgetotwn University |
11266178 |
39 |
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
Kyoto University |
11266177 |
26 |
The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding. |
Kyoto University |
11206480 |
6 |
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C. |
Institute of Organic Chemistry |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
11012021 |
69 |
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. |
Basf Bioresearch |
10966739 |
28 |
Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C. |
National Cancer Institute-Bethesda |
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 |
10762046 |
7 |
Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones. |
National Cancer Institute-Bethesda |
10743939 |
63 |
Synthesis and biological activities of NB-506 analogues modified at the glucose group. |
Banyu Tsukuba Research Institute |
10715158 |
31 |
Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C? |
National Cancer Institute-Bethesda |
30530196 |
32 |
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
Gachon University |
10612598 |
29 |
4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70. |
Celltech Therapeutics |
10612590 |
56 |
Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
31298542 |
108 |
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. |
Chinese Academy of Sciences |
10514283 |
8 |
Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores. |
Seoul National University |
31417666 |
55 |
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. |
Vertex Pharmaceuticals |
10397502 |
36 |
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes. |
Stanford University |
10360738 |
5 |
Synthesis and protein kinase C binding activity of benzolactam-V7. |
Institute of Organic Chemistry |
10340602 |
100 |
Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506. |
Banyu Tsukuba Research Institute |
10090785 |
63 |
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. |
Novartis |
10021922 |
10 |
Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety. |
University of Tokyo |
31693351 |
473 |
Discovery of 4 |
TBA |
31343875 |
34 |
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents. |
Toho University |
9873742 |
5 |
Conformationally constrained analogues of diacylglycerol (DAG). 15. The indispensable role of the sn-1 and sn-2 carbonyls in the binding of DAG-lactones to protein kinase C (PK-C). |
National Institutes of Health |
30733087 |
53 |
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
China Pharmaceutical University |
9873429 |
6 |
Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement. |
National Cancer Institute-Bethesda |
9341921 |
7 |
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group. |
Université |
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 |
9135029 |
29 |
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity. |
Georgetown University Medical Center |
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 |
8960550 |
5 |
Conformationally constrained analogues of diacylglycerol. 13. Protein kinase C ligands based on templates derived from 2,3-dideoxy-L-erythro(threo)-hexono-1,4-lactone and 2-deoxyapiolactone. |
National Cancer Institute-Bethesda |
8893841 |
23 |
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
Université |
8709095 |
87 |
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
Eli Lilly |
8691423 |
89 |
4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase. |
Ciba Pharmaceuticals |
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 |
8568825 |
13 |
Conformationally constrained analogues of diacylglycerol. 12. Ultrapotent protein kinase C ligands based on a chiral 4,4-disubstituted heptono-1,4-lactone template. |
National Cancer Institute-Bethesda |
8568819 |
6 |
Conformationally constrained analogues of diacylglycerol. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template. |
National Cancer Institute-Bethesda |
8568806 |
9 |
Conformationally constrained analogues of diacylglycerol. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template. |
National Cancer Institute-Bethesda |
8176711 |
18 |
Protein kinase C. Modeling of the binding site and prediction of binding constants. |
National Cancer Institute-Bethesda |
23803585 |
7 |
Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities. |
Kyoto University |
7799398 |
5 |
The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies. |
National Cancer Institute-Bethesda |
21388717 |
1 |
Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG. |
University of Milan |
7807122 |
4 |
New cytotoxic peroxylactones from the marine sponge, Plakinastrella onkodes. |
Harbor Branch Oceanographic Institution |
9834165 |
5 |
Isolation and structure elucidation of new PKCalpha inhibitors from Pinus flexilis. |
Virginia Polytechnic and State University |
17618015 |
13 |
Bioactive peroxides as potential therapeutic agents. |
The Hebrew University of Jerusalem |
11334563 |
5 |
Computational analysis of PKA-balanol interactions. |
University of California At San Diego |
10753478 |
11 |
Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry. |
The City University of New York |
10052965 |
9 |
Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent. |
Universit£ |
9572888 |
4 |
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle. |
Universit£ |
14505650 |
12 |
An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury. |
Northwestern University |
27731641 |
5 |
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes. |
Kaohsiung Medical University |
30274941 |
36 |
A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model. |
Astellas Pharma |
29135244 |
5 |
Natural Products with Heteroatom-Rich Ring Systems. |
University of Auckland |
29558119 |
30 |
Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. |
Zhejiang University |
30026041 |
139 |
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition. |
University College Cork |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
29545102 |
159 |
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor. |
Merck |
29870245 |
39 |
Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties. |
University of Colorado |
29688013 |
81 |
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors. |
Agency For Science, Technology and Research (A*Star) |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29860841 |
140 |
?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands. |
Seoul National University |
29853332 |
50 |
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration. |
Universit£ |
28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
28699740 |
294 |
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. |
Takeda Pharmaceutical |
28991459 |
71 |
Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism. |
Dongguk University |
28478927 |
46 |
Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors. |
Martin-Luther-University Halle-Wittenberg |
28392275 |
24 |
Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKC?, PKC?, and RasGRP. |
National Institute of Industrial Technology |
27943581 |
8 |
Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products. |
The University of Sydney |
27128528 |
42 |
Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects. |
Harvard Medical School |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
11121615 |
32 |
Synthesis and in vitro opioid activity profiles of DALDA analogues. |
Clinical Research Institute of Montreal |
18804034 |
9 |
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. |
Duke University Medical Center |
17585751 |
48 |
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
Amgen |
16236500 |
26 |
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors. |
Johnson & Johnson Pharmaceutical |
16279769 |
28 |
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives. |
Sapienza University of Rome |
15689148 |
19 |
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. |
Shanghai Institute of Materia Medica |
15664516 |
21 |
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases. |
University of Dundee |
15026054 |
55 |
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. |
Cnrs |
| 127 |
DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS |
Parke-Davis Pharmaceutical Research |