Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00008

Target Information
NameVascular endothelial growth factor receptor 2    
Type of targetSuccessful target    
SynonymsFetal liver kinase 1    
Kinase NYK    
Kinase insert domain receptor    
Protein-tyrosine kinase receptor Flk-1    
VEGFR-2    
DiseaseAngiogenesis[1]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[2]
Drug(s)Pazopanib HClApprovedRenal cell carcinoma[3]
RegorafenibApprovedMetastatic colorectal cancer
SunitinibLaunchedAdvanced renal cell carcinoma[4][5][6][7]
Sunitinib malatePhase IVMetastatic Renal Cell Carcinoma; Gastrointestinal Stromal Tumors[8][9][6]
ASP4130US Filed; Europe Phase-IIIAdvanced renal cell carcinoma
AxitinibPhase IIIRenal Cell Carcinoma[6][8][10]
CabozantinibPhase IIIMedullary Thyroid Cancer[11]
CediranibPhase IIIFallopian Tube Cancer; Ovarian Cancer; Peritoneal Cavity Cancer[6][12]
MotesanibPhase IIINon-small cell lung cancer[13][14][15]
PazopanibPhase IIIAdvanced / metastatic renal cancer[6][16][17]
RamucirumabPhase IIIA variety of cancers, such as metastatic breast, colorectal and gastric cancers
VandetanibPhase IIISolid tumours, NSCLC[6][12]
PazopanibPhase II completedSolid tumours, NSCLC[6][16][17]
XL647Phase II completedCarcinoma, Non-Small-Cell Lung[18]
AfliberceptPhase IIOvarian cancer[19]
AxitinibPhase IILung Cancer; Thyroid Cancer[6][8][10]
CP-547632Phase IINSCLC, ovarian cancer, solid tumours[6][20]
CabozantinibPhase IIBreast Cancer, Gastric/GE Junctional Cancer, Hepatocellular Carcinoma, Melanoma, Castration-Resistant Prostate Cancer, Non-small Cell Lung Cancer, Ovarian Cancer, Pancreatic Cancer, Small Cell Lung Cance[11]
CabozantinibPhase IIMetastatic Castration-Resistant Prostate Cancer, Ovarian Cancer[11]
CediranibPhase IIAdvanced Breast Cancer[6][12]
MotesanibPhase IIBreast cancer[13][14][15]
PTK787/ZK 222584Phase IIGlioma, solid tumours, NSCLC[6][21]
PegdinetanibPhase IINSCLC
SU-14813Phase IIMetastatic breast cancer[6][8][22]
SunitinibPhase IIAdvanced renal cell carcinoma[4][5][6][7]
Sunitinib malatePhase IISoft Tissue Sarcoma[8][9][6]
VandetanibPhase IIBreast, thyroid tumours, multiple myeloma, brain, head & neck cancer[6][12]
XL880Phase IIGastric Cancer, Renal Cell Carcinoma, Squamous Cell Cancer of the Head and Neck[23][24][25][26][16]
PF-00337210Phase I completedSolid Tumors
XL647Phase I completedCancer[18]
CabozantinibPhase IbDifferentiated Thyroid Cancer, Renal Cell Carcinoma[11]
4SC-203Phase ISolid tumors[27]
BAY-57-9352Phase IVarious cancers[6]
CT-322Phase ICancer/Tumors[28]
CediranibPhase IColorectal cancer[6][12]
E 7080Phase IOvarian cancer[19]
KRN633Phase IGlioma & solid tumours[6]
Motesanib diphosphatePhase IProgressive non-small cell lung cancer[29][14]
OSI-930Phase IVarious cancers[6]
PTK787/ZK 222584Phase IAML, ovarian, myelodysplastic syndrome, prostate cancer[6][21]
SU-14813Phase IVarious Cancers[6][8][22]
XL880Phase ISolid Tumors[23][24][25][26][16]
XL999Phase IAdvanced Malignancies[25]
CEP-7055Discontinued in Phase IPancreastic cancer, prostate cancer & solid tumours[6]
CYC116Terminated in Phase ISolid Tumors[30]
PTK787/ZK 222584Discontinued in Phase IIICancer, colorectal; Cancer, renal; Cancer, brain; Cancer, breast; Cancer, ovarian; Cancer, pancreatic; Cancer, prostate; Cancer, lung, non-small cell; Macular degeneration, age-related, wet[6][21]
SU-6668DiscontinuedAdvanced solid tumours[6][31]
CT-322PreclinicalMacular Degeneration[28]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayCytokine-cytokine receptor interaction
Focal adhesion
VEGF signaling pathway
UniProt IDP35968
PDB Structure1VR2; 1Y6A; 1Y6B; 1YWN; 2OH4; 2P2H; 2P2I; 2QU5; 2QU6; 2RL5; 2X1W; 2X1X; 2XIR; 3B8Q; 3B8R; 3BE2; 3C7Q; 3CJF; 3CJG; 3CP9; 3CPB; 3CPC; 3DTW; 3EFL; 3EWH; 3KVQ; 3S35; 3S36; 3S37; 3U6J; 3VHE; 3VHK; 3VID; 3VNT; 3VO3; 4AG8; 4AGC; 4AGD; 4ASD; 4ASE.    
FunctionReceptor for VEGF or VEGF-c, and has a tyrosine-protein kinase activity. the VEGF-kinase ligand/receptor signaling system plays a key role in vascular development and regulation of vascular permeability.    
SequenceMQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (+)K-252a[32]
(2-Methoxy-phenyl)-[33]
(3-Phenoxy-phenyl)-[33]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine[34]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine[33]
2- (1H-indazol-3-yl)-1H-benzo[d]imidazole[35]
2- (5-Phenyl-oxazol-2-ylamino)-benzonitrile[33]
2- (p-toluidino)-4-phenylpyrimidine-5-carbonitrile[36]
2- (pyrimidin-4-ylamino)thiazole-5-carbonitrile[37]
3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione[38]
3,4-diphenyl-1H-pyrrole-2,5-dione[38]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine[39]
3- ([40]
3- (1H-Indol-2-yl)-1H-quinolin-2-one[41]
3- (4-aminophenyl)thieno[3,2-c]pyridin-4-amine[42]
3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione[38]
3- (5-Phenyl-oxazol-2-ylamino)-benzonitrile[33]
3- (5-Thiophen-3-yl-pyridin-3-yl)-1H-indole[43]
3-Benzimidazol-2-ylhydroquinolin-2-one[44]
3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide[45]
3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole[46]
4- (4-aminophenyl)-1H-indazol-3yl-amine[47]
4- (4-m-Tolylamino-phthalazin-1-yl)-benzamide[48]
4- (4-p-Tolylamino-phthalazin-1-yl)-benzamide[48]
4- (5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide[33]
4- (isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine[49]
4- (isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine[49]
4-Chloro-N- (2-chloro-benzoyl)-benzenesulfonamide[50]
4-Chloro-N- (2-methyl-benzoyl)-benzenesulfonamide[50]
4-Chloro-N- (3-chloro-benzoyl)-benzenesulfonamide[50]
4-Chloro-N- (4-chloro-benzoyl)-benzenesulfonamide[50]
4-Chloro-N- (4-nitro-benzoyl)-benzenesulfonamide[50]
4-phenyl-2- (phenylamino)pyrimidine-5-carbonitrile[36]
4SC-203[27]
5- (4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole[51]
6- (1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one[41]
6-o-tolylquinazolin-2-amine[52]
8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one[40]
AAL-993[53]
AG1295[54]
AZD-1152-HQPA,   Barasertib[55]
Aflibercept[19]
Axitinib[6][8][10]
BAY-57-9352[6]
BMS-536924[56]
BMS-540215[57]
BMS-645737[58]
CB-676475[59]
CEP-5104[60]
CEP-7055[6]
CP-547632[6][20]
CT-322[28]
CYC116[30]
Cabozantinib[11]
Cediranib[6][12]
E 7080[19]
IM-023911[48]
IM-094261[48]
IM-094882[49]
Isoindolinone Urea derivative[61]
K-252a analogue[62]
K-252a analogue[62]
K-252a analogue[62]
K-252a analogue[62]
K-252a analogue[62]
K-252a analogue[62]
K-252a analogue[62]
KRN633[6]
L000021649[39]
Motesanib[13][14][15]
Motesanib diphosphate[29][14]
N- (2,4-Dichloro-benzoyl)-benzenesulfonamide[50]
N- (3-Bromo-benzoyl)-4-chloro-benzenesulfonamide[50]
NERATINIB[63]
OSI-930[6]
PD-153035[63]
PD-173074[64]
PTK787/ZK 222584[6][21]
Pazopanib[6][16][17]
Pazopanib HCl[3]
Phenyl- (5-phenyl-oxazol-2-yl)-amine[33]
Ro-4396686[65]
SEMAXINIB[53]
SU-11652[66]
SU-14813[6][8][22]
SU-5402[40]
SU-5416[67]
SU-6668[6][31]
Sunitinib[4][5][6][7]
Sunitinib malate[8][9][6]
TG-100435[68]
VATALANIB[63]
Vandetanib[6][12]
WHI-P180[40]
XL647[18]
XL880[23][24][25][26][16]
XL999[25]
[3- (5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol[33]
AntibodyIMC-1C11[69]
Multitarget4SC-203[27]
Aflibercept[19]
Axitinib[6][8][10]
BAY-57-9352[6]
CEP-7055[6]
CYC116[30]
Cabozantinib[11]
Motesanib[13][14][15]
Motesanib diphosphate[29][14]
OSI-930[6]
Pazopanib[6][16][17]
Pazopanib HCl[3]
SU-6668[6][31]
Sunitinib[4][5][6][7]
Sunitinib malate[8][9][6]
Vandetanib[6][12]
XL647[18]
XL880[23][24][25][26][16]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Inhibition of vascular endothelial growth factor (VEGF) as a novel approach for cancer therapy. Medicina (B Aires). 2000;60 Suppl 2:41-7. To Reference
Ref 2Overexpression of vascular endothelial growth factor (VEGF) and its cellular receptor KDR (VEGFR-2) in the bone marrow of patients with acute myeloid leukemia. Leukemia. 2002 Jul;16(7):1302-10. To Reference
Ref 3Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 4FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat. 2009 Jun;12(3):81-9. Epub 2009 May 20. To Reference
Ref 5FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro. Cancer Res. 2009 Apr 1;69(7):3032-41. Epub 2009 Mar 24. To Reference
Ref 6A 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. To Reference
Ref 7Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 8Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 9Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. Epub 2008 Oct 29. To Reference
Ref 10Pfizer. Report of Pfizer. July 28 2008. To Reference
Ref 112011 Pipeline of Exelixis. To Reference
Ref 12AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 13Amgen. Product Development Pipeline. February 6 2009. To Reference
Ref 14Phase 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. Epub 2009 Jun 29. To Reference
Ref 15Amgen. Report of Amgen. 2009. To Reference
Ref 16GSK. Product Development Pipeline. February 2009. To Reference
Ref 17Pazopanib, a VEGF receptor tyrosine kinase inhibitor for cancer therapy. Curr Opin Investig Drugs. 2008 Dec;9(12):1324-35. To Reference
Ref 18Combined inhibition of vascular endothelial growth factor and epidermal growth factor signaling in non-small-cell lung cancer therapy. Clin Lung Cancer. 2009 Mar;10 Suppl 1:S17-23. To Reference
Ref 19Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36. To Reference
Ref 20YM-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. To Reference
Ref 21Additive effect of PTK787/ZK 222584, a potent inhibitor of VEGFR phosphorylation, with Idarubicin in the treatment of acute myeloid leukemia. Exp Hematol. 2009 Jun;37(6):679-91. To Reference
Ref 22SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. To Reference
Ref 23Pipeline of EXELIXIS. EXELIXIS. 2009 To Reference
Ref 24MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20932-7. Epub 2007 Dec 18. To Reference
Ref 25Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73. To Reference
Ref 262011 Pipeline of Exelixis. To Reference
Ref 272011 Pipeline of 4SC AG. To Reference
Ref 28The Adnectin CT-322 is a novel VEGF receptor 2 inhibitor that decreases tumor burden in an orthotopic mouse model of pancreatic cancer. BMC Cancer. 2008 Nov 27;8:352. To Reference
Ref 29Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 30Report from Cyclacel Pharmaceuticals. Cyclacel Limited. April 2008 To Reference
Ref 31Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. To Reference
Ref 32J Med Chem. 2007 Feb 8;50(3):433-41.Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a. To Reference
Ref 33J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. To Reference
Ref 34Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. To Reference
Ref 35Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. To Reference
Ref 36Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. To Reference
Ref 37Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. Epub 2005 Dec 20.Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase. To Reference
Ref 38J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference
Ref 39Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41.Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. To Reference
Ref 40Bioorg Med Chem Lett. 2007 Apr 15;17(8):2126-33. Epub 2007 Feb 2.Pharmacophore modeling and in silico screening for new KDR kinase inhibitors. To Reference
Ref 41Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5.Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding. To Reference
Ref 42Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.Thienopyridine urea inhibitors of KDR kinase. To Reference
Ref 43Bioorg Med Chem Lett. 2003 Sep 15;13(18):2973-6.Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors. To Reference
Ref 44J Med Chem. 2009 Jan 22;52(2):278-92.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. To Reference
Ref 45Bioorg Med Chem Lett. 2006 Jan 1;16(1):96-9. Epub 2005 Oct 10.Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. To Reference
Ref 46Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. Epub 2006 Jun 5.Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. To Reference
Ref 47J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.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. To Reference
Ref 48Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. To Reference
Ref 49Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. Epub 2005 Dec 28.Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II. To Reference
Ref 50J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. To Reference
Ref 51Bioorg Med Chem Lett. 2003 Aug 4;13(15):2485-8.Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. To Reference
Ref 52J Med Chem. 2006 Sep 21;49(19):5671-86.Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. To Reference
Ref 53J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. To Reference
Ref 54Bioorg Med Chem. 2009 Oct 15;17(20):7324-36. Epub 2009 Aug 22.Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors. To Reference
Ref 55J Med Chem. 2007 May 3;50(9):2213-24. Epub 2007 Mar 21.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. To Reference
Ref 56J Med Chem. 2005 Sep 8;48(18):5639-43.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 antitumor activity. To Reference
Ref 57J Med Chem. 2006 Apr 6;49(7):2143-6.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. To Reference
Ref 58Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. Epub 2008 Mar 22.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. To Reference
Ref 59Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. Epub 2005 Oct 10.Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. To Reference
Ref 60J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. To Reference
Ref 61Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9.Isoindolinone ureas: a novel class of KDR kinase inhibitors. To Reference
Ref 62J Med Chem. 2005 Jun 2;48(11):3776-83.Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity. To Reference
Ref 63Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. To Reference
Ref 64J Med Chem. 2005 Jul 14;48(14):4628-53.Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. To Reference
Ref 65Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. To Reference
Ref 66J Med Chem. 2003 Mar 27;46(7):1116-9.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 tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 67Results of a Phase I dose-escalating study of the antiangiogenic agent, SU5416, in patients with advanced malignancies. Clin Cancer Res. 2002 Sep;8(9):2798-805. To Reference
Ref 68Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.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 kinase inhibitor with anti-tumor activity in preclinical assays. To Reference
Ref 69Technology evaluation: IMC-1C11, ImClone Systems. Curr Opin Mol Ther. 2001 Aug;3(4):418-24. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543