The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28159414 |
15 |
The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity. |
Osaka Prefecture University |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
27856237 |
11 |
Synthesis, anticancer, and docking studies of salicyl-hydrazone analogues: A novel series of small potent tropomyosin receptor kinase A inhibitors. |
Dongguk University |
27779399 |
22 |
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain. |
Eli Lilly |
27299736 |
37 |
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. |
St. John'S University |
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 |
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 |
26995531 |
32 |
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit. |
The University Of Tokyo |
26771245 |
7 |
Recent developments of 2-aminothiazoles in medicinal chemistry. |
Sree Chaitanya College |
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 |
26442778 |
15 |
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors. |
Institute For Basic Science (Ibs) |
26431428 |
36 |
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). |
Wuxi Apptec |
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 |
26121481 |
37 |
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿. |
Vertex Pharmaceuticals |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute Of The Novartis Research Foundation |
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 |
25791677 |
15 |
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges. |
Zhengzhou University |
25723005 |
111 |
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. |
TBA |
25454499 |
6 |
Design and nuclear magnetic resonance (NMR) structure determination of the second extracellular immunoglobulin tyrosine kinase A (TrkAIg2) domain construct for binding site elucidation in drug discovery. |
Southmead Hospital |
25068800 |
34 |
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. |
University Of North Carolina At Chapel Hill |
25022204 |
78 |
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. |
Universit£ |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
24914455 |
38 |
Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain. |
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 |
24819116 |
135 |
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo |
Pfizer |
24432909 |
13 |
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
Pfizer |
24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
24900767 |
3 |
Inhibitors of Tropomyosin-Receptor Kinases (Trk's): Potential Pain Therapy and More. |
Therachem Research Medilab (India) |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23742252 |
81 |
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase |
Genomics Institute Of The Novartis Research Foundation |
23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
21381769 |
56 |
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
Universite£ |
23061660 |
92 |
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. |
Genentech |
22827572 |
67 |
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). |
Glaxosmithkline |
22039836 |
188 |
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141). |
Johnson & Johnson Pharmaceutical Research & Development |
24900538 |
27 |
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. |
TBA |
22575050 |
40 |
Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities. |
Korea Advanced Institute Of Science And Technology (Kaist) |
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 |
24900443 |
158 |
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. |
TBA |
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 |
21608528 |
166 |
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. |
Merck Research Laboratories |
21138246 |
44 |
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. |
Astrazeneca R&D |
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 |
19716697 |
110 |
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II. |
Boehringer Ingelheim Pharmaceuticals |
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 |
19320489 |
125 |
Discovery and development of aurora kinase inhibitors as anticancer agents. |
Vertex Pharmaceuticals |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
18508265 |
13 |
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone. |
Cephalon |
18342505 |
43 |
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
11931608 |
17 |
Inhibition of protein-protein association by small molecules: approaches and progress. |
Pfizer |
15013000 |
31 |
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. |
Glaxosmithkline |
22040023 |
63 |
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). |
Pfizer |
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 |
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 |
22001029 |
28 |
Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors. |
Korea Research Institute Of Chemical Technology |
21958544 |
31 |
Indolin-2-one p38a inhibitors III: bioisosteric amide replacement. |
RhôNe-Poulenc Rorer |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21812414 |
106 |
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
Pfizer |
21493067 |
22 |
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. |
Astrazeneca R&D Boston |
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 |
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 |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
19039322 |
50 |
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
Center For Molecular Medicine Of The Austrian Academy Of Sciences |
20655209 |
18 |
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. |
Université |
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 |
20382527 |
26 |
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. |
Bristol-Myers Squibb Research And Development |
20361800 |
22 |
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. |
Institute Of Science And Technology |
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 |
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 |
19857966 |
62 |
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors. |
Astrazeneca R&D Boston |
18289854 |
44 |
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase. |
Bristol-Myers Squibb Research And Development |
18242992 |
30 |
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. |
Johnson & Johnson Pharmaceutical Research & Development |
18055203 |
51 |
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA. |
Bristol-Myers Squibb Research And Development |
17239587 |
43 |
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors. |
Cephalon |
15916429 |
11 |
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity. |
Cephalon |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
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 |
12270156 |
8 |
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a. |
Cephalon |
11755341 |
50 |
Mixed lineage kinase activity of indolocarbazole analogues. |
Kyowa Hakko Kogyo |
9191963 |
12 |
Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives. |
Kyowa Hakko Kogyo |
29518312 |
78 |
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer. |
Nankai University |
28465100 |
85 |
Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors. |
Merck |
23009660 |
17 |
Structure-activity relationships of bergenin derivatives effect on a-glucosidase inhibition. |
Kinki University |
22524677 |
6 |
Interaction of superoxide dismutase with the glycine zipper regions of ß-amyloid peptides: is there an implication towards Alzheimer's disease and oxidative stress? |
Rhodes University |
23884422 |
10 |
Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation. |
Mcgill University |
27496071 |
4 |
Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents. |
Korea Institute Of Science And Technology |
15665139 |
3 |
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2. |
German Cancer Research Center |
9928251 |
27 |
Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor. |
Albany Medical College |
16611213 |
6 |
Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction. |
Johnson & Johnson Pharmaceutical Research & Development |
21566738 |
3 |
Virtual screening for potential inhibitors of homology modeled Leptospira interrogans MurD ligase. |
Svims University |
1320204 |
1 |
Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285. |
Centre De Pharmacologie-Endocrinologie (Montpellier, France) |
20426425 |
2 |
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237. |
University Of Sheffield |
18851976 |
4 |
Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles. |
University Of Milano |
18440229 |
175 |
2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors. |
Irbm/Merck Research Laboratories |
15482949 |
17 |
Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties. |
Glaxosmithkline |
9876115 |
183 |
Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. |
University Of Auckland |