The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28541695 |
192 |
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
East China University of Science and Technology |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
27750146 |
58 |
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
Chinese Academy of Sciences |
27914362 |
54 |
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
The First Affiliated Hospital of Zhengzhou University |
28190652 |
26 |
Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
27573544 |
43 |
Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design. |
Taiwan National Health Research Institutes |
27299736 |
37 |
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. |
St. John'S University |
27348537 |
60 |
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
East China University of Science & Technology |
27131066 |
36 |
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Chinese Academy of Sciences |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
26881908 |
13 |
De Novo Design at the Edge of Chaos. |
Swiss Federal Institute of Technology (Eth) |
27106711 |
87 |
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2). |
Green Valley Research Institute |
26717201 |
68 |
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. |
Shenyang Pharmaceutical University |
26698536 |
56 |
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
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 |
26396681 |
58 |
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. |
Novartis Institutes For Biomedical Research |
26526740 |
111 |
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
Univ. Lille |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
25908516 |
10 |
Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties. |
Sichuan University |
25827399 |
52 |
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis. |
Chinese Academy of Sciences |
25474320 |
10 |
Nintedanib: from discovery to the clinic. |
Boehringer Ingelheim Pharma |
25086238 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
Shenyang Pharmaceutical University |
24785465 |
80 |
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
Chinese Academy of Sciences |
25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
25589926 |
20 |
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase. |
Astex Pharmaceuticals |
25462265 |
2 |
Design, synthesis and in vitro antitumor activity of novel N-substituted-4-phenyl/benzylphthalazin-1-ones. |
Egyptian Russian University |
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 |
25440879 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents. |
Shenyang Pharmaceutical University |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
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 |
24900886 |
66 |
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors. |
Chinese Academy of Sciences |
24565969 |
69 |
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
Chinese Academy of Sciences |
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 |
23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
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 |
23375090 |
54 |
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents. |
Duquesne University |
23268742 |
11 |
Bioassay-guided isolation of proanthocyanidins with antiangiogenic activities. |
Universit£ |
23414235 |
12 |
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp. |
Institute of Microbial Chemistry (Bikaken) |
22765894 |
223 |
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
Exelixis |
23127890 |
96 |
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. |
Exelixis |
23123015 |
22 |
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors. |
Takeda Pharmaceutical |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
23098265 |
46 |
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
University of Genoa |
22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
National Institute of Biological Sciences |
22980219 |
55 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy. |
Takeda Pharmaceutical |
22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
22726931 |
113 |
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
National Health Research Institutes |
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 |
22439974 |
79 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders. |
Takeda Pharmaceutical |
22372864 |
25 |
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. |
Hanmi Research Center |
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 |
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 |
20570525 |
56 |
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase. |
Chinese Academy of Sciences |
20420387 |
118 |
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. |
Glaxosmithkline |
20092323 |
23 |
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents. |
Duquesne University |
20000469 |
179 |
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase. |
Boehringer Ingelheim Pharmaceuticals |
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 |
19522465 |
102 |
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
Boehringer Ingelheim Pharma |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
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 |
18324761 |
65 |
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation. |
Amgen |
18324759 |
133 |
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors. |
Amgen |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
18023347 |
74 |
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors. |
Abbott Laboratories |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
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 |
12477352 |
85 |
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
Novartis Pharma |
22370340 |
91 |
N¿?¿-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation. |
Duquesne University |
21888439 |
7 |
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. |
Pfizer |
22169262 |
26 |
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase. |
Shenyang Pharmaceutical University |
22204741 |
46 |
N¿?¿-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors. |
Duquesne University |
22078412 |
4 |
Disulfide and amide-bridged cyclic peptide analogues of the VEGF8¿?¿9¿? fragment: synthesis, conformational analysis and biological evaluation. |
Instituto De Qu£Mica M£Dica |
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 |
22003817 |
71 |
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. |
Takeda Pharmaceutical |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
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 |
21665484 |
37 |
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold. |
Chinese Academy of Sciences |
21708468 |
101 |
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
National Health Research Institutes |
21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
21517068 |
45 |
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity. |
East China University of Science and Technology |
21405128 |
47 |
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent. |
Chinese Academy of Sciences |
21349728 |
12 |
Parallel solid-phase synthesis of a small library of linear and hydrocarbon-bridged analogues of VEGF(81-91): potential biological tools for studying the VEGF/VEGFR-1 interaction. |
Instituto De Qu£Mica M£Dica |
21316232 |
41 |
4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II. |
Johnson & Johnson Pharmaceutical Research & Development |
21273066 |
83 |
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation. |
National University of Ireland |
20932747 |
61 |
The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. |
Ansaris |
20833055 |
44 |
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation. |
Takeda Pharmaceutical |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
18559524 |
21 |
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
Boehringer Ingelheim Austria |
16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
20472445 |
23 |
Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
Ewha Womans University |
20462213 |
6 |
Biochemical and structural analysis of the binding determinants of a vascular endothelial growth factor receptor peptidic antagonist. |
University of Paris |
20430619 |
73 |
8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors. |
Cephalon |
20403700 |
76 |
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. |
Duquesne University |
20403693 |
60 |
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines. |
Duquesne University |
20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
19854647 |
17 |
Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo. |
Astrazeneca |
20031417 |
40 |
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers. |
Hadassah Hebrew University Hospital |
20148563 |
42 |
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. |
The Institute of Cancer Research |
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 |
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 |
19188066 |
102 |
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2. |
Decode |
19124243 |
108 |
3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2. |
Decode |
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 |
18691885 |
60 |
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. |
Ariad Pharmaceuticals |
18676144 |
93 |
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable. |
Astrazeneca |
18640036 |
71 |
Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors. |
Imclone Systems |
18610999 |
24 |
Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening. |
Institute of Materia Medica |
18557606 |
64 |
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
18467105 |
71 |
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents. |
Duquesne University |
17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
18308565 |
70 |
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases. |
Cephalon |
17900101 |
3 |
Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor. |
Université |
17827009 |
116 |
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors. |
Tanabe Research Laboratories Usa |
17826090 |
9 |
On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition. |
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 |
17499505 |
78 |
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
17481893 |
146 |
Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates. |
Chemical Diversity |
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 |
17289388 |
8 |
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors. |
Tibotec |
17239587 |
43 |
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors. |
Cephalon |
17188873 |
225 |
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2. |
Chemical Diversity |
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 |
16759855 |
130 |
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
16750628 |
47 |
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. |
Abbott Laboratories |
16735117 |
50 |
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases. |
Abbott Laboratories |
16603352 |
89 |
Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. |
Chiron |
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 |
16446087 |
76 |
Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases. |
Chiron |
16366598 |
51 |
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. |
Johnson & Johnson Pharmaceutical Research and Development |
16364640 |
79 |
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases. |
Chemical Diversity |
16321531 |
86 |
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II. |
Chemical Diversity |
16216503 |
5 |
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. |
Korea Research Institute of Chemical Technology |
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 |
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 |
14684289 |
81 |
Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity. |
Pfizer |
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 |
12941313 |
20 |
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. |
Novartis Pharma |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
32305182 |
48 |
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
Shenyang Pharmaceutical University |
31818631 |
13 |
Exploring structure-promiscuity relationships using dual-site promiscuity cliffs and corresponding single-site analogs. |
Rheinische Friedrich-Wilhelms-Universit£T |
32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
27448775 |
102 |
Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase. |
Shanghai Pharmaceuticals Holding |
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 |
31284081 |
60 |
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
National Research Centre |
30856407 |
2 |
Structural studies of the binding of an antagonistic cyclic peptide to the VEGFR1 domain 2. |
Universit£ |
29522671 |
80 |
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
Chinese Academy of Sciences |
31693351 |
473 |
Discovery of 4 |
TBA |
30620194 |
12 |
Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
Albert Ludwigs University Freiburg |
30744932 |
11 |
Discovery of novel thienoquinoline-2-carboxamide chalcone derivatives as antiproliferative EGFR tyrosine kinase inhibitors. |
Al-Azhar University |
31401008 |
34 |
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review. |
Y. B. Chavan College of Pharmacy |
31079967 |
43 |
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors. |
School of Marine Science and Technology |
30763817 |
39 |
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach. |
University of Naples Federico Ii |
30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
31513411 |
41 |
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
Korea University |
30600149 |
35 |
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton. |
University of South China |
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 |
30342424 |
6 |
Tau Tubulin Kinase 1 (TTBK1), a new player in the fight against neurodegenerative diseases. |
Centro De Investigaciones Biol�Gicas-Csic |
31670517 |
41 |
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms. |
West China Hospital of Sichuan University |
31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
31306818 |
19 |
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
Fuzhou University |
26509640 |
234 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. |
Abbvie Bioresearch Center |
30978288 |
113 |
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
Northwestern University |
18474428 |
25 |
Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety. |
The University of Tokushima |
15481975 |
62 |
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. |
Eli Lilly |
30096580 |
19 |
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity. |
Al-Azhar University |
29775937 |
52 |
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
Chinese Academy of Sciences |
28844802 |
4 |
Recent developments in small molecule therapies for renal cell carcinoma. |
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif) |
28760313 |
5 |
Recent advances (2015-2016) in anticancer hybrids. |
University of Kwazulu Natal |
30480444 |
85 |
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model. |
Sichuan University/Collaborative Innovation Center of Biotherapy |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
29549836 |
47 |
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
Universit£ |
29266937 |
36 |
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy? |
University of South Australia |
29787262 |
64 |
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously. |
Shandong University |
29894944 |
66 |
Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
China Pharmaceutical University |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29032031 |
91 |
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors. |
Xi'An Jiaotong University |
29102175 |
91 |
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4. |
Xi'An Jiaotong University |
29357250 |
80 |
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. |
China Pharmaceutical University |
28686443 |
7 |
Identification of Peptidic Antagonists of Vascular Endothelial Growth Factor Receptor 1 by Scanning the Binding Epitopes of Its Ligands. |
Umr 8638 Cnrs |
28956923 |
34 |
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. |
Chinese Academy of Sciences |
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 |
28411455 |
45 |
Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization. |
Shanghai Pharmaceuticals Holding |
28714692 |
232 |
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
University of Chinese Academy of Sciences |
21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
24379401 |
5 |
A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer. |
Universität Duisburg-Essen |
11909603 |
1 |
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. |
Takeda Chemical Industries |
9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
1353247 |
71 |
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. |
University of Nebraska |
1321043 |
17 |
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist. |
UniversitÉ |
15634023 |
50 |
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. |
Institut Claudius Regaud |
18266314 |
65 |
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5. |
Institut De Biologie Structurale |
16632353 |
14 |
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. |
Abbott Laboratories |
16289938 |
24 |
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification. |
Vernalis (R&D) |
16913714 |
4 |
Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance. |
Purdue University |
12767917 |
30 |
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates. |
St. Mary'S Hospital |
10479289 |
55 |
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization. |
Rhone-Poulenc Rorer |