Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T80975
(Former ID: TTDS00008)
|
||||
Target Name |
Vascular endothelial growth factor receptor 2 (KDR)
|
||||
Synonyms |
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
|
||||
Gene Name |
KDR
|
||||
Target Type |
Successful target
|
[1] | |||
Disease | [+] 8 Target-related Diseases | + | |||
1 | Breast cancer [ICD-11: 2C60-2C6Y] | ||||
2 | Colorectal cancer [ICD-11: 2B91] | ||||
3 | Malignant digestive organ neoplasm [ICD-11: 2C11] | ||||
4 | Renal cell carcinoma [ICD-11: 2C90] | ||||
5 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | ||||
6 | Stomach cancer [ICD-11: 2B72] | ||||
7 | Thrombocytopenia [ICD-11: 3B64] | ||||
8 | Thyroid cancer [ICD-11: 2D10] | ||||
Function |
Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC. Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD.
|
||||
BioChemical Class |
Kinase
|
||||
UniProt ID | |||||
EC Number |
EC 2.7.10.1
|
||||
Sequence |
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD
WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV |
||||
Drugs and Modes of Action | |||||
Approved Drug(s) | [+] 11 Approved Drugs | + | |||
1 | Axitinib | Drug Info | Approved | Renal cell carcinoma | [2], [3], [4] |
2 | Cabozantinib | Drug Info | Approved | Thyroid cancer | [5], [6] |
3 | Lenvatinib | Drug Info | Approved | Thyroid cancer | [7] |
4 | Pazopanib HCl | Drug Info | Approved | Renal cell carcinoma | [8] |
5 | Ramucirumab | Drug Info | Approved | Gastric adenocarcinoma | [9], [10] |
6 | Regorafenib | Drug Info | Approved | Metastatic colorectal cancer | [11], [3] |
7 | Romiplostim | Drug Info | Approved | Thrombocytopenia | [12], [13] |
8 | Sorafenib | Drug Info | Approved | Renal cell carcinoma | [14], [15] |
9 | Sunitinib | Drug Info | Approved | Gastrointestinal cancer | [16], [17], [18] |
10 | Vandetanib | Drug Info | Approved | Solid tumour/cancer | [19], [20] |
11 | YN-968D1 | Drug Info | Approved | Breast cancer | [21], [22], [23] |
Clinical Trial Drug(s) | [+] 33 Clinical Trial Drugs | + | |||
1 | Brivanib | Drug Info | Phase 3 | Liver cancer | [24], [25] |
2 | Cediranib | Drug Info | Phase 3 | Peritoneal cavity cancer | [26], [27] |
3 | E-3810 | Drug Info | Phase 3 | Solid tumour/cancer | [28], [29] |
4 | Fruquintinib | Drug Info | Phase 3 | Solid tumour/cancer | [30] |
5 | HKI-272 | Drug Info | Phase 3 | Breast cancer | [31], [32] |
6 | Rivoceranib | Drug Info | Phase 3 | Gastric adenocarcinoma | [32] |
7 | Rosiglitazone + metformin | Drug Info | Phase 3 | Diabetic complication | [33] |
8 | Tivozanib | Drug Info | Phase 3 | Renal cell carcinoma | [34], [35] |
9 | Alacizumab pegol | Drug Info | Phase 2 | Non-small-cell lung cancer | [36] |
10 | BAY-57-9352 | Drug Info | Phase 2 | Solid tumour/cancer | [37] |
11 | BMS-690514 | Drug Info | Phase 2 | Chronic pain | [38] |
12 | CP-547632 | Drug Info | Phase 2 | Solid tumour/cancer | [39], [40] |
13 | Delphinidin | Drug Info | Phase 2 | Cardiovascular disease | [41] |
14 | Famitinib | Drug Info | Phase 2 | Solid tumour/cancer | [42], [43] |
15 | RAF265 | Drug Info | Phase 2 | Melanoma | [44], [45] |
16 | VATALANIB | Drug Info | Phase 2 | Solid tumour/cancer | [46], [47] |
17 | XL880 | Drug Info | Phase 2 | Squamous head and neck cell carcinom | [48], [49] |
18 | Anti-VEGFR2 CD8 cell therapy | Drug Info | Phase 1/2 | Solid tumour/cancer | [50] |
19 | Elpamotide | Drug Info | Phase 1/2 | Biliary cancer | [51] |
20 | MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [52] |
21 | OTSGC-A24 | Drug Info | Phase 1/2 | Colorectal cancer | [53] |
22 | Altiratinib | Drug Info | Phase 1 | Solid tumour/cancer | [54] |
23 | CEP-11981 | Drug Info | Phase 1 | Solid tumour/cancer | [55], [56] |
24 | CYC116 | Drug Info | Phase 1 | Solid tumour/cancer | [57] |
25 | E-7050 | Drug Info | Phase 1 | Head and neck cancer | [58], [59] |
26 | KRN633 | Drug Info | Phase 1 | Solid tumour/cancer | [60], [61] |
27 | OSI-930 | Drug Info | Phase 1 | Solid tumour/cancer | [62], [63] |
28 | Pegdinetanib | Drug Info | Phase 1 | Non-small-cell lung cancer | [64] |
29 | PF-00337210 | Drug Info | Phase 1 | Solid tumour/cancer | [65] |
30 | PLX-4720 | Drug Info | Phase 1 | Cutaneous melanoma | [66] |
31 | Sulfatinib | Drug Info | Phase 1 | Solid tumour/cancer | [67] |
32 | TAK-593 | Drug Info | Phase 1 | Solid tumour/cancer | [68] |
33 | XL999 | Drug Info | Phase 1 | Advanced malignancy | [18] |
Patented Agent(s) | [+] 1 Patented Agents | + | |||
1 | Antibodie derivative 10 | Drug Info | Patented | Neoplasm | [69], [70] |
Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | |||
1 | Motesanib | Drug Info | Discontinued in Phase 3 | Non-small-cell lung cancer | [71], [72] |
2 | SU-14813 | Drug Info | Discontinued in Phase 2 | Breast cancer | [73], [74] |
3 | IMC-1C11 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [75] |
4 | CEP-5214 | Drug Info | Terminated | Solid tumour/cancer | [76] |
Mode of Action | [+] 4 Modes of Action | + | |||
Modulator | [+] 17 Modulator drugs | + | |||
1 | Axitinib | Drug Info | [3], [4] | ||
2 | Ramucirumab | Drug Info | [10] | ||
3 | Regorafenib | Drug Info | [78] | ||
4 | Sorafenib | Drug Info | [15], [80] | ||
5 | Sunitinib | Drug Info | [17], [81] | ||
6 | Brivanib | Drug Info | [85] | ||
7 | Tivozanib | Drug Info | [90] | ||
8 | Delphinidin | Drug Info | [41] | ||
9 | RAF265 | Drug Info | [94] | ||
10 | XL880 | Drug Info | [85] | ||
11 | Anti-VEGFR2 CD8 cell therapy | Drug Info | [50], [95] | ||
12 | E-7050 | Drug Info | [100] | ||
13 | OSI-930 | Drug Info | [62], [63] | ||
14 | Pegdinetanib | Drug Info | [101] | ||
15 | PF-00337210 | Drug Info | [102] | ||
16 | TAK-593 | Drug Info | [68], [104] | ||
17 | EPI-0030 | Drug Info | [101] | ||
Inhibitor | [+] 104 Inhibitor drugs | + | |||
1 | Cabozantinib | Drug Info | [6], [77] | ||
2 | Lenvatinib | Drug Info | [1] | ||
3 | Pazopanib HCl | Drug Info | [8] | ||
4 | Romiplostim | Drug Info | [79] | ||
5 | Vandetanib | Drug Info | [82], [83] | ||
6 | YN-968D1 | Drug Info | [84] | ||
7 | Cediranib | Drug Info | [82], [83] | ||
8 | E-3810 | Drug Info | [86] | ||
9 | Fruquintinib | Drug Info | [87] | ||
10 | HKI-272 | Drug Info | [88] | ||
11 | Rosiglitazone + metformin | Drug Info | [82], [89] | ||
12 | BAY-57-9352 | Drug Info | [82] | ||
13 | BMS-690514 | Drug Info | [92] | ||
14 | CP-547632 | Drug Info | [82], [93] | ||
15 | Famitinib | Drug Info | [43] | ||
16 | VATALANIB | Drug Info | [88] | ||
17 | MK-2461 | Drug Info | [52] | ||
18 | CEP-11981 | Drug Info | [82] | ||
19 | CYC116 | Drug Info | [99] | ||
20 | KRN633 | Drug Info | [82] | ||
21 | PLX-4720 | Drug Info | [81] | ||
22 | Sulfatinib | Drug Info | [103] | ||
23 | XL999 | Drug Info | [105] | ||
24 | Pyridine derivative 18 | Drug Info | [106] | ||
25 | Pyrimidine derivative 12 | Drug Info | [69] | ||
26 | Pyrimidine derivative 13 | Drug Info | [69] | ||
27 | Pyrimidine derivative 14 | Drug Info | [69] | ||
28 | Pyrimidine derivative 4 | Drug Info | [69] | ||
29 | Quinazoline derivative 15 | Drug Info | [106] | ||
30 | Quinazoline derivative 16 | Drug Info | [106] | ||
31 | Quinoline and quinazoline derivative 1 | Drug Info | [69] | ||
32 | Motesanib | Drug Info | [107], [108], [109] | ||
33 | SU-14813 | Drug Info | [82], [110], [111] | ||
34 | AG1295 | Drug Info | [113] | ||
35 | (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [115] | ||
36 | (3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [115] | ||
37 | (4-Phenoxy-phenyl)-quinazolin-4-yl-amine | Drug Info | [116] | ||
38 | (5-Phenyl-oxazol-2-yl)-m-tolyl-amine | Drug Info | [115] | ||
39 | 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole | Drug Info | [117] | ||
40 | 2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [115] | ||
41 | 2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile | Drug Info | [118] | ||
42 | 2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile | Drug Info | [119] | ||
43 | 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione | Drug Info | [120] | ||
44 | 3,4-diphenyl-1H-pyrrole-2,5-dione | Drug Info | [120] | ||
45 | 3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine | Drug Info | [121] | ||
46 | 3-((3-bromothiophen-2-yl)methylene)indolin-2-one | Drug Info | [122] | ||
47 | 3-(1H-Indol-2-yl)-1H-quinolin-2-one | Drug Info | [123] | ||
48 | 3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine | Drug Info | [124] | ||
49 | 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione | Drug Info | [120] | ||
50 | 3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [115] | ||
51 | 3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole | Drug Info | [125] | ||
52 | 3-Benzimidazol-2-ylhydroquinolin-2-one | Drug Info | [126] | ||
53 | 3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide | Drug Info | [127] | ||
54 | 3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole | Drug Info | [128] | ||
55 | 4-(4-aminophenyl)-1H-indazol-3yl-amine | Drug Info | [129] | ||
56 | 4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide | Drug Info | [130] | ||
57 | 4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide | Drug Info | [130] | ||
58 | 4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide | Drug Info | [115] | ||
59 | 4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine | Drug Info | [131] | ||
60 | 4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine | Drug Info | [131] | ||
61 | 4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
62 | 4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
63 | 4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
64 | 4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
65 | 4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
66 | 4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile | Drug Info | [118] | ||
67 | 4-[3-Hydroxyanilino]-6,7-Dimethoxyquinazoline | Drug Info | [122] | ||
68 | 5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole | Drug Info | [133] | ||
69 | 6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one | Drug Info | [123] | ||
70 | 6-o-tolylquinazolin-2-amine | Drug Info | [134] | ||
71 | 8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one | Drug Info | [122] | ||
72 | AAL-993 | Drug Info | [79] | ||
73 | AG-E-85378 | Drug Info | [135] | ||
74 | AMG-429 | Drug Info | [101] | ||
75 | AST-487 | Drug Info | [136] | ||
76 | BIBF-1202 | Drug Info | [137] | ||
77 | BMS-536924 | Drug Info | [138] | ||
78 | BMS-645737 | Drug Info | [139] | ||
79 | BX-795 | Drug Info | [140] | ||
80 | BX-912 | Drug Info | [140] | ||
81 | CB-676475 | Drug Info | [141] | ||
82 | CEP-5104 | Drug Info | [142] | ||
83 | IM-023911 | Drug Info | [130] | ||
84 | IM-094261 | Drug Info | [130] | ||
85 | IM-094882 | Drug Info | [131] | ||
86 | Indolin-2-one deriv. 4b | Drug Info | [143] | ||
87 | Isoindolinone Urea derivative | Drug Info | [144] | ||
88 | JNJ-38158471 | Drug Info | [101] | ||
89 | K-252a analogue | Drug Info | [145] | ||
90 | Ki-20227 | Drug Info | [146] | ||
91 | L000021649 | Drug Info | [121] | ||
92 | MG-516 | Drug Info | [101] | ||
93 | N-(2,4-Dichloro-benzoyl)-benzenesulfonamide | Drug Info | [132] | ||
94 | N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide | Drug Info | [132] | ||
95 | Phenyl-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [115] | ||
96 | PMID22765894C8h | Drug Info | [147] | ||
97 | PMID23639540C13a | Drug Info | [148] | ||
98 | PP121 | Drug Info | [149] | ||
99 | Pyrazolo[1,5-a]pyrimidine 3G | Drug Info | [121] | ||
100 | Ro-4396686 | Drug Info | [150] | ||
101 | SU-11652 | Drug Info | [151] | ||
102 | TG-100435 | Drug Info | [152] | ||
103 | VEGF receptor 2 kinase inhibitor I | Drug Info | [153] | ||
104 | [3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol | Drug Info | [115] | ||
Antagonist | [+] 3 Antagonist drugs | + | |||
1 | Altiratinib | Drug Info | [98] | ||
2 | Rivoceranib | Drug Info | [32] | ||
3 | CEP-5214 | Drug Info | [114] | ||
Binder | [+] 1 Binder drugs | + | |||
1 | Antibodie derivative 6 | Drug Info | [69] | ||
Target Regulators | |||||
Target-regulating microRNAs | |||||
Target-interacting Proteins | |||||
Target Profiles in Patients | |||||
Target Expression Profile (TEP) | |||||
Target Affiliated Biological Pathways | |||||
KEGG Pathway | [+] 8 KEGG Pathways | + | |||
1 | Ras signaling pathway | ||||
2 | Rap1 signaling pathway | ||||
3 | Cytokine-cytokine receptor interaction | ||||
4 | Endocytosis | ||||
5 | PI3K-Akt signaling pathway | ||||
6 | VEGF signaling pathway | ||||
7 | Focal adhesion | ||||
8 | Proteoglycans in cancer | ||||
NetPath Pathway | [+] 1 NetPath Pathways | + | |||
1 | IL2 Signaling Pathway | ||||
Panther Pathway | [+] 2 Panther Pathways | + | |||
1 | Angiogenesis | ||||
2 | VEGF signaling pathway | ||||
PID Pathway | [+] 9 PID Pathways | + | |||
1 | HIF-2-alpha transcription factor network | ||||
2 | Beta3 integrin cell surface interactions | ||||
3 | Signaling events mediated by TCPTP | ||||
4 | SHP2 signaling | ||||
5 | S1P1 pathway | ||||
6 | VEGF and VEGFR signaling network | ||||
7 | Integrins in angiogenesis | ||||
8 | Signaling events mediated by VEGFR1 and VEGFR2 | ||||
9 | Notch-mediated HES/HEY network | ||||
Reactome | [+] 6 Reactome Pathways | + | |||
1 | Neurophilin interactions with VEGF and VEGFR | ||||
2 | VEGF binds to VEGFR leading to receptor dimerization | ||||
3 | Integrin cell surface interactions | ||||
4 | EPHA-mediated growth cone collapse | ||||
5 | VEGFA-VEGFR2 Pathway | ||||
6 | VEGFR2 mediated cell proliferation | ||||
WikiPathways | [+] 5 WikiPathways | + | |||
1 | Focal Adhesion | ||||
2 | Nifedipine Activity | ||||
3 | Cardiac Progenitor Differentiation | ||||
4 | Signaling by VEGF | ||||
5 | Angiogenesis | ||||
Target-Related Models and Studies | |||||
Target Validation | |||||
Target QSAR Model | |||||
References | |||||
REF 1 | Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36. | ||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5659). | ||||
REF 3 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | ||||
REF 4 | Axitinib: VEGF inhibition in advanced thyroid cancer. Lancet Oncol. 2014 Jul;15(8):e310. | ||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5887). | ||||
REF 6 | Clinical pipeline report, company report or official report of Exelixis (2011). | ||||
REF 7 | FDA Approved Drug Products from FDA Official Website. 2018. Application Number: (ANDA) 208627. | ||||
REF 8 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | ||||
REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7390). | ||||
REF 10 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | ||||
REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5891). | ||||
REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6974). | ||||
REF 13 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | ||||
REF 14 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5711). | ||||
REF 15 | Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. | ||||
REF 16 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5713). | ||||
REF 17 | 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101. | ||||
REF 18 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. | ||||
REF 19 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5717). | ||||
REF 20 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | ||||
REF 21 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7648). | ||||
REF 22 | Clinical pipeline report, company report or official report of LSK BioPharma. | ||||
REF 23 | ClinicalTrials.gov (NCT02426034) Study of Apatinib Tablets in the Treatment of Advanced or Metastatic Gastric Cancer. U.S. National Institutes of Health. | ||||
REF 24 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5671). | ||||
REF 25 | ClinicalTrials.gov (NCT01108705) Comparison of Brivanib and Best Supportive Care (BSC) With Placebo and BSC for Treatment of Liver Cancer in Asian Patients Who Have Failed Sorafenib Treatment. U.S. National Institutes of Health. | ||||
REF 26 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5664). | ||||
REF 27 | ClinicalTrials.gov (NCT02446600) Olaparib or Cediranib Maleate and Olaparib Compared With Standard Platinum-Based Chemotherapy in Treating Patients With Recurrent Platinum-Sensitive Ovarian, Fallopian Tube, or Primary Peritoneal Cancer. U.S. National Institutes of Health. | ||||
REF 28 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7649). | ||||
REF 29 | ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health. | ||||
REF 30 | ClinicalTrials.gov (NCT02314819) A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients RESCO). U.S. National Institutes of Health. | ||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154) | ||||
REF 32 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
REF 33 | ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health. | ||||
REF 34 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6058). | ||||
REF 35 | ClinicalTrials.gov (NCT01076010) An Extension Treatment Protocol for Subjects Who Have Participated in a Phase 3 Study of Tivozanib Versus Sorafenib in Renal Cell Carcinoma (Protocol AV-951-09-301). U.S. National Institutes of Health. | ||||
REF 36 | ClinicalTrials.gov (NCT00152477) A Study of Paclitaxel/Carboplatin With or Without CDP791 in Patients With Lung Cancer. U.S. National Institutes of Health. | ||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605) | ||||
REF 38 | A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62. | ||||
REF 39 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7881). | ||||
REF 40 | ClinicalTrials.gov (NCT00096239) CP-547,632 in Treating Patients With Recurrent or Persistent Ovarian Cancer, Primary Peritoneal Cancer, or Fallopian Tube Cancer. U.S. National Institutes of Health. | ||||
REF 41 | Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96. | ||||
REF 42 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7886). | ||||
REF 43 | Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706. | ||||
REF 44 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5674). | ||||
REF 45 | ClinicalTrials.gov (NCT00304525) A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma. U.S. National Institutes of Health. | ||||
REF 46 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5705). | ||||
REF 47 | ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health. | ||||
REF 48 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5679). | ||||
REF 49 | Clinical pipeline report, company report or official report of Exelixis (2011). | ||||
REF 50 | ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health. | ||||
REF 51 | ClinicalTrials.gov (NCT00655785) Antiangiogenic Peptide Vaccine Therapy With Gemcitabine in Treating Patient With Pancreatic Cancer (Phase1/2). U.S. National Institutes of Health. | ||||
REF 52 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
REF 53 | ClinicalTrials.gov (NCT01227772) Study of OTSGC-A24 Vaccine in Advanced Gastric Cancer. U.S. National Institutes of Health. | ||||
REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040094) | ||||
REF 55 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8189). | ||||
REF 56 | ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
REF 57 | ClinicalTrials.gov (NCT00560716) A Phase I Pharmacologic Study of CYC116, an Oral Aurora Kinase Inhibitor, in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
REF 58 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7956). | ||||
REF 59 | ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers. | ||||
REF 60 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6057). | ||||
REF 61 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017407) | ||||
REF 62 | OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74. | ||||
REF 63 | Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9. | ||||
REF 64 | ClinicalTrials.gov (NCT01146171) Japanese Phase 1 Study of BMS-844203 (CT322). U.S. National Institutes of Health. | ||||
REF 65 | ClinicalTrials.gov (NCT01105533) A Dose Finding Study Of A New Medication, PF-00337210 That Will Possibly Decrease Blood Supply To Tumors. U.S. National Institutes of Health. | ||||
REF 66 | Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. Oncologist. 2011;16(3):296-309. | ||||
REF 67 | ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
REF 68 | Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013Apr;104(4):486-94. | ||||
REF 69 | VEGFR-2 inhibitors and the therapeutic applications thereof: a patent review (2012-2016).Expert Opin Ther Pat. 2017 Sep;27(9):987-1004. | ||||
REF 70 | Microsomal prostaglandin E2 synthase-1 inhibitors: a patent review.Expert Opin Ther Pat. 2017 Sep;27(9):1047-1059. | ||||
REF 71 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5660). | ||||
REF 72 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011016) | ||||
REF 73 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5712). | ||||
REF 74 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021861) | ||||
REF 75 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013121) | ||||
REF 76 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016567) | ||||
REF 77 | Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751. | ||||
REF 78 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
REF 79 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. | ||||
REF 80 | Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40. | ||||
REF 81 | In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. | ||||
REF 82 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. | ||||
REF 83 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | ||||
REF 84 | YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80. | ||||
REF 85 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | ||||
REF 86 | E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. | ||||
REF 87 | Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. | ||||
REF 88 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. | ||||
REF 89 | Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. | ||||
REF 90 | Clinical pipeline report, company report or official report of AVEO Pharmaceuticals. | ||||
REF 91 | Phase I evaluation of CDP791, a PEGylated di-Fab' conjugate that binds vascular endothelial growth factor receptor 2. Clin Cancer Res. 2007 Dec 1;13(23):7113-8. | ||||
REF 92 | Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93. | ||||
REF 93 | YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. | ||||
REF 94 | RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications. Invest New Drugs. 2013 Feb;31(1):200-5. | ||||
REF 95 | Vascular normalizing doses of antiangiogenic treatment reprogram the immunosuppressive tumor microenvironment and enhance immunotherapy. Proc Natl Acad Sci U S A. 2012 Oct 23;109(43):17561-6. | ||||
REF 96 | Clinical phase I study of elpamotide, a peptide vaccine for vascular endothelial growth factor receptor 2, in patients with advanced solid tumors. Cancer Sci. 2012 Dec;103(12):2135-8. | ||||
REF 97 | J Clin Oncol 33, 2015 (suppl 3; abstr 65). | ||||
REF 98 | Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals. | ||||
REF 99 | Clinical pipeline report, company report or official report of Cyclacel. | ||||
REF 100 | E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5. | ||||
REF 101 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1813). | ||||
REF 102 | Inhibition of VEGFR-2 Reverses Type 1 Diabetes in NOD Mice by Abrogating Insulitis and Restoring Islet Function. Diabetes. 2013 August; 62(8): 2870-2878. | ||||
REF 103 | Clinical pipeline report, company report or official report of Hutchison Medi Pharma. | ||||
REF 104 | Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51. | ||||
REF 105 | Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73. | ||||
REF 106 | RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99. | ||||
REF 107 | Clinical pipeline report, company report or official report of Amgen (2009). | ||||
REF 108 | Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. | ||||
REF 109 | Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8. | ||||
REF 110 | Pfizer. Product Development Pipeline. March 31 2009. | ||||
REF 111 | SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. | ||||
REF 112 | Technology evaluation: IMC-1C11, ImClone Systems. Curr Opin Mol Ther. 2001 Aug;3(4):418-24. | ||||
REF 113 | Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase i... Bioorg Med Chem. 2009 Oct 15;17(20):7324-36. | ||||
REF 114 | Neuropilin-2 interacts with VEGFR-2 and VEGFR-3 and promotes human endothelial cell survival and migration. Blood. 2006 Aug 15;108(4):1243-50. | ||||
REF 115 | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9. | ||||
REF 116 | Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. | ||||
REF 117 | Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. | ||||
REF 118 | 4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. | ||||
REF 119 | Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. | ||||
REF 120 | Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81. | ||||
REF 121 | Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharm... Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41. | ||||
REF 122 | Pharmacophore modeling and in silico screening for new KDR kinase inhibitors. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2126-33. | ||||
REF 123 | Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmaco... Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5. | ||||
REF 124 | Thienopyridine urea inhibitors of KDR kinase. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. | ||||
REF 125 | Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors. Bioorg Med Chem Lett. 2003 Sep 15;13(18):2973-6. | ||||
REF 126 | Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor... J Med Chem. 2009 Jan 22;52(2):278-92. | ||||
REF 127 | Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. Bioorg Med Chem Lett. 2006 Jan 1;16(1):96-9. | ||||
REF 128 | Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. | ||||
REF 129 | 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 ... J Med Chem. 2007 Apr 5;50(7):1584-97. | ||||
REF 130 | Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8. | ||||
REF 131 | Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. | ||||
REF 132 | Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. J Med Chem. 2004 Oct 21;47(22):5367-80. | ||||
REF 133 | Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2485-8. | ||||
REF 134 | Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86. | ||||
REF 135 | Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6003-8. | ||||
REF 136 | The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64. | ||||
REF 137 | Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. | ||||
REF 138 | Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43. | ||||
REF 139 | 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]t... Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. | ||||
REF 140 | Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. | ||||
REF 141 | Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. | ||||
REF 142 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9. | ||||
REF 143 | Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases. J Med Chem. 2000 Jul 13;43(14):2655-63. | ||||
REF 144 | Isoindolinone ureas: a novel class of KDR kinase inhibitors. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9. | ||||
REF 145 | Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on tr... J Med Chem. 2005 Jun 2;48(11):3776-83. | ||||
REF 146 | A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43. | ||||
REF 147 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
REF 148 | Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52. | ||||
REF 149 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
REF 150 | Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. | ||||
REF 151 | Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9. | ||||
REF 152 | Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. | ||||
REF 153 | Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Wang and Dr. Li.