The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27077705 |
4 |
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
Chinese Academy Of Sciences |
| 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 |
| 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 |
| 26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
| 26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
| 26102506 |
40 |
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
Celgene |
| 26083478 |
66 |
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
Celgene |
| 26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute Of The Novartis Research Foundation |
| 25822739 |
37 |
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents. |
Ku Leuven |
| 25589926 |
20 |
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase. |
Astex Pharmaceuticals |
| 25369270 |
93 |
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. |
Galapagos |
| 25221654 |
39 |
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors. |
Novartis Institutes For Biomedical Research |
| 24904961 |
27 |
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
Qilu Pharmaceutical |
| 24417566 |
43 |
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
Icahn School Of Medicine At Mount Sinai |
| 24900776 |
75 |
Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability. |
Array Biopharma |
| 24138939 |
112 |
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors. |
Janssen Research And Development |
| 23937569 |
22 |
Selectivity data: assessment, predictions, concordance, and implications. |
Eli Lilly |
| 23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
| 23498918 |
41 |
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. |
Takeda Pharmaceutical |
| 23414803 |
9 |
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. |
Celgene |
| 23219325 |
36 |
Novel cinnoline-based inhibitors of LRRK2 kinase activity. |
Elan Pharmaceuticals |
| 21429745 |
49 |
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß. |
Glaxosmithkline |
| 19303774 |
87 |
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3. |
Glaxosmithkline |
| 17194588 |
92 |
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. |
Glaxosmithkline |
| 23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
| 24900421 |
87 |
Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. |
TBA |
| 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 |
| 24900482 |
32 |
Targeted kinase selectivity from kinase profiling data. |
TBA |
| 22452518 |
22 |
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. |
Sichuan University |
| 22339472 |
148 |
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth |
S Bio |
| 22168626 |
32 |
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. |
Ambit Biosciences |
| 22497760 |
144 |
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases. |
Astrazeneca |
| 22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
| 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 |
| 20570147 |
25 |
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 20156689 |
5 |
Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
University Of Newcastle |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 18789685 |
172 |
Kinase array design, back to front: biaryl amides. |
Glaxosmithkline |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 18495479 |
25 |
Structure-based optimization of a potent class of arylamide FMS inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 18324761 |
65 |
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation. |
Amgen |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University Of Oxford |
| 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 |
| 18023347 |
74 |
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors. |
Abbott Laboratories |
| 18289848 |
35 |
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 12477352 |
85 |
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
Novartis Pharma |
| 12238930 |
94 |
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. |
Kyowa Hakko Kogyo |
| 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 |
| 16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
| 22153662 |
137 |
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. |
Astrazeneca |
| 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 |
| 22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 20630752 |
40 |
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors. |
Millennium Pharmaceuticals |
| 21316232 |
41 |
4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II. |
Johnson & Johnson Pharmaceutical Research & Development |
| 20925433 |
21 |
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
Aristotle University Of Thessaloniki |
| 20817538 |
16 |
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
Novartis Institutes For Biomedical Research |
| 20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 20681538 |
61 |
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile. |
Development Center For Biotechnology |
| 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 |
| 20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
| 20137931 |
9 |
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode. |
Pfizer |
| 19646870 |
34 |
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors. |
Ambit Biosciences |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 19754199 |
29 |
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
Ambit Biosciences |
| | 46 |
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4- |
TBA |
| 19114305 |
14 |
3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile. |
Astrazeneca R&D Boston |
| 19113866 |
129 |
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. |
Novartis Institutes For Biomedical Research |
| 19112018 |
46 |
Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase. |
Astrazeneca R&D Boston |
| 19097792 |
24 |
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity. |
Astrazeneca R&D Boston |
| 18818075 |
25 |
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors. |
Glaxosmithkline |
| 18723346 |
26 |
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors. |
Amgen |
| 18694641 |
32 |
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer. |
Astrazeneca R&D Boston |
| 18691885 |
60 |
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. |
Ariad Pharmaceuticals |
| 18651728 |
1 |
Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity. |
Epicept |
| 18557606 |
64 |
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
| 18242992 |
30 |
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. |
Johnson & Johnson Pharmaceutical Research & Development |
| 17904845 |
70 |
Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents. |
Johnson And Johnson Pharmaceutical Research And Development |
| 17870531 |
46 |
Synthesis of novel anilinoquinolines as c-fms inhibitors. |
Glaxosmithkline |
| 17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
| 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 |
| 17425296 |
161 |
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel. |
Abbott Laboratories |
| 17391959 |
100 |
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
| 17343372 |
143 |
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. |
Abbott Laboratories |
| 15771417 |
48 |
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors. |
Johnson & Johnson Pharmaceutical Research And Development |
| 12086491 |
116 |
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. |
Pharmaceutical Research Institute |
| 9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
| 8278895 |
52 |
Evaluation of 5-[18F]fluoropropylepidepride as a potential PET radioligand for imaging dopamine D2 receptors. |
Vanderbilt University |
| 19549076 |
26 |
Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes. |
Universita Degli Studi Di Firenze |
| 12144928 |
11 |
Sequencing, modeling, and selective inhibition of Trypanosoma brucei hexokinase. |
Universite Paul Sabatier |
| 11983334 |
6 |
Aminoglycosides modified by resistance enzymes display diminished binding to the bacterial ribosomal aminoacyl-tRNA site. |
Wayne State University |
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