The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28039836 |
41 |
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. |
East China Normal University |
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 |
27839918 |
28 |
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). |
Takeda California |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang 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 |
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 |
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 |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan 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 |
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 |
25988399 |
126 |
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1. |
Argenta Discovery |
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 |
25699576 |
42 |
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
University of South Florida |
25594740 |
33 |
Identification of novel aminothiazole and aminothiadiazole conjugated cyanopyridines as selective CHK1 inhibitors. |
Cairo University |
25771484 |
5 |
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold. |
Zhejiang University |
25047935 |
2 |
Design of granulatimide and isogranulatimide analogues as potential Chk1 inhibitors: Study of amino-platforms for their synthesis. |
Universit£ |
25042558 |
38 |
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors. |
Zhejiang University |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
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 |
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 |
25453805 |
18 |
Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1. |
Genentech |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
24904961 |
27 |
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
Qilu Pharmaceutical |
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 |
23906342 |
14 |
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. |
Takeda Pharmaceutical |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
24091081 |
49 |
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach. |
Merck Research Laboratories |
24007918 |
6 |
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway. |
University of Edinburgh Cancer Research Centre In The Institute of Genetics and Molecular Medicine |
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 |
23602398 |
43 |
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. |
Merck Research Laboratories |
23517069 |
1 |
Therapeutic agents triggering nonapoptotic cancer cell death. |
Texas State University-San Marcos |
23587425 |
37 |
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors. |
Merck Research Laboratories |
23535330 |
83 |
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. |
Merck Research Laboratories |
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 |
23362959 |
72 |
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo. |
Sichuan University |
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 |
19385614 |
303 |
Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes. |
Abbott Laboratories |
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 |
22883026 |
34 |
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives. |
Takeda Pharmaceutical |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
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 |
22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
22809559 |
31 |
Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide. |
Universit£ |
24900442 |
51 |
Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode. |
TBA |
22503250 |
128 |
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity. |
Amri |
24900358 |
69 |
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. |
TBA |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
22374217 |
33 |
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates. |
Merck Research Laboratories |
22365762 |
64 |
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity. |
Merck Research Laboratories |
22342147 |
55 |
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors. |
Astrazeneca R&D Boston |
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 |
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 |
20000735 |
12 |
Through the"gatekeeper door": exploiting the active kinase conformation. |
Nerviano Medical Sciences |
20022510 |
61 |
Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2. |
The Institute of Cancer Research |
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 |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
17360485 |
10 |
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. |
Millennium Pharmaceuticals |
18321713 |
9 |
Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles. |
Universit£ |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
18358720 |
44 |
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors. |
Abbott Laboratories |
18191399 |
57 |
Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases. |
University of Auckland |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
17827013 |
55 |
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors. |
Abbott Laboratories |
17887663 |
34 |
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors. |
Pfizer |
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 |
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 |
22285028 |
22 |
Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors. |
Michigan State University |
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 |
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 |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
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 |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20630752 |
40 |
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors. |
Millennium 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 |
21391610 |
139 |
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. |
Vertex Pharmaceuticals |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
21186793 |
72 |
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. |
The Institute of Cancer Research |
21094608 |
74 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1. |
Merck Research Laboratories |
21094607 |
66 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2. |
Merck Research Laboratories |
21074424 |
57 |
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors. |
Merck Research Laboratories |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
20943405 |
11 |
Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as check point 1 kinase inhibitors. |
Hokkaido University |
20936789 |
56 |
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. |
The Institute of Cancer Research |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20674356 |
41 |
Synthesis of selenophene derivatives as novel CHK1 inhibitors. |
Development Center For Biotechnology |
20673630 |
38 |
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration. |
Astrazeneca R&D Boston |
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 |
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 |
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 |
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 |
19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth Research |
19854645 |
87 |
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. |
Wyeth Research |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19775160 |
79 |
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability. |
Takeda Pharmaceutical |
19338355 |
104 |
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
University of Illinois At Chicago |
19155174 |
20 |
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors. |
Merck Research Laboratories |
19111462 |
23 |
Synthesis and CHK1 inhibitory potency of Hymenialdisine analogues. |
Institut De Recherche Servier |
19097792 |
24 |
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity. |
Astrazeneca R&D Boston |
18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
18602198 |
1 |
A three-step synthesis from rebeccamycin of an efficient checkpoint kinase 1 inhibitor. |
Université |
18547806 |
100 |
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors. |
Astrazeneca R&D Boston |
18342518 |
6 |
Novel 5-azaindolocarbazoles as cytotoxic agents and Chk1 inhibitors. |
Université |
17869387 |
158 |
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases. |
University of Auckland |
17502122 |
7 |
Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of pyrrolo[3,4-a]carbazole-1,3-diones, pyrrolo[3,4-c]carbazole-1,3-diones, and 2-aminopyridazino[3,4-a]pyrrolo[3,4-c]carbazole-1,3,4,7-tetraone. |
Université |
17931867 |
42 |
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors. |
Abbott Laboratories |
17900896 |
44 |
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase. |
Merck Research Laboratories |
17804227 |
28 |
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors. |
Merck Research Laboratories |
17768051 |
28 |
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability. |
Abbott Laboratories |
17722905 |
16 |
Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide. |
Université |
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 |
17582773 |
8 |
Synthesis and biological activities of isogranulatimide analogues. |
Université |
17544271 |
49 |
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors. |
Abbott Laboratories |
17490879 |
38 |
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies. |
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 |
16990002 |
45 |
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors. |
Merck Research Laboratories |
16884302 |
209 |
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. |
University of Auckland |
16603354 |
15 |
4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors. |
Chiron |
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 |
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 |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
29016121 |
44 |
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3. |
Novartis Institutes For Biomedical Research |
27658802 |
41 |
Overview of the SAMPL5 host-guest challenge: Are we doing better? |
University of California San Diego |
| 298 |
ERK2 in CSAR_FULL_RELEASE_3JULY2012 |
Csar |
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 |
16492149 |
16 |
Structure-based optimization of MurF inhibitors. |
Abbott Laboratories |
19309082 |
53 |
Discovering potent inhibitors against the beta-hydroxyacyl-acyl carrier protein dehydratase (FabZ) of Helicobacter pylori: structure-based design, synthesis, bioassay, and crystal structure determination. |
Shanghai Institute of Materia Medica |
16600594 |
23 |
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design. |
Johnson & Johnson Pharmaceutical |
19317447 |
37 |
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
Kochi Medical School |