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TargetVascular endothelial growth factor receptor 2
LigandBDBM50377352
Substrate/Competitorn/a
Meas. Tech.ChEMBL_479558 (CHEMBL929422)
IC50 53±n/a nM
Citation Ruel, RThibeault, CL'Heureux, AMartel, ACai, ZWWei, DQian, LBarrish, JCMathur, AD'Arienzo, CHunt, JTKamath, AMarathe, PZhang, YDerbin, GWautlet, BMortillo, SJeyaseelan, RHenley, BTejwani, RBhide, RSTrainor, GLFargnoli, JLombardo, LJ 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. Bioorg Med Chem Lett18:2985-9 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Vascular endothelial growth factor receptor 2
Name:Vascular endothelial growth factor receptor 2
Synonyms:Flk-1 | Flk1 | Kdr | VEGFR-2 (KDR) | VGFR2_MOUSE | Vascular endothelial growth factor receptor 2
Type:PROTEIN
Mol. Mass.:152506.58
Organism:Mus musculus
Description:ChEMBL_1469997
Residue:1367
Sequence:
MESKALLAVALWFCVETRAASVGLPGDFLHPPKLSTQKDILTILANTTLQITCRGQRDLD
WLWPNAQRDSEERVLVTECGGGDSIFCKTLTIPRVVGNDTGAYKCSYRDVDIASTVYVYV
RDYRSPFIASVSDQHGIVYITENKNKTVVIPCRGSISNLNVSLCARYPEKRFVPDGNRIS
WDSEIGFTLPSYMISYAGMVFCEAKINDETYQSIMYIVVVVGYRIYDVILSPPHEIELSA
GEKLVLNCTARTELNVGLDFTWHSPPSKSHHKKIVNRDVKPFPGTVAKMFLSTLTIESVT
KSDQGEYTCVASSGRMIKRNRTFVRVHTKPFIAFGSGMKSLVEATVGSQVRIPVKYLSYP
APDIKWYRNGRPIESNYTMIVGDELTIMEVTERDAGNYTVILTNPISMEKQSHMVSLVVN
VPPQIGEKALISPMDSYQYGTMQTLTCTVYANPPLHHIQWYWQLEEACSYRPGQTSPYAC
KEWRHVEDFQGGNKIEVTKNQYALIEGKNKTVSTLVIQAANVSALYKCEAINKAGRGERV
ISFHVIRGPEITVQPAAQPTEQESVSLLCTADRNTFENLTWYKLGSQATSVHMGESLTPV
CKNLDALWKLNGTMFSNSTNDILIVAFQNASLQDQGDYVCSAQDKKTKKRHCLVKQLIIL
ERMAPMITGNLENQTTTIGETIEVTCPASGNPTPHITWFKDNETLVEDSGIVLRDGNRNL
TIRRVRKEDGGLYTCQACNVLGCARAETLFIIEGAQEKTNLEVIILVGTAVIAMFFWLLL
VILVRTVKRANEGELKTGYLSIVMDPDELPLDERCERLPYDASKWEFPRDRLKLGKPLGR
GAFGQVIEADAFGIDKTATCKTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLL
GACTKPGGPLMVIVEFSKFGNLSTYLRGKRNEFVPYKSKGARFRQGKDYVGELSVDLKRR
LDSITSSQSSASSGFVEEKSLSDVEEEEASEELYKDFLTLEHLICYSFQVAKGMEFLASR
KCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVY
TIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDC
WHEDPNQRPSFSELVEHLGNLLQANAQQDGKDYIVLPMSETLSMEEDSGLSLPTSPVSCM
EEEEVCDPKFHYDNTAGISHYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDSQTDSGM
VLASEELKTLEDRNKLSPSFGGMMPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSD
EAGLLKMVDAAVHADSGTTLQLTSCLNGSGPVPAPPPTPGNHERGAA
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  Blast E-value cutoff:
BDBM50377352
n/a
NameBDBM50377352
Synonyms:BMS-645737 | CHEMBL261592
TypeSmall organic molecule
Emp. Form.C20H20N8O
Mol. Mass.388.4258
SMILESCC(C)c1c(cn2ncnc(Nc3cnc4[nH]c(C)cc4c3)c12)-c1nnc(C)o1
Structure
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