Reaction Details |
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Target | Vascular endothelial growth factor receptor 2 |
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Ligand | BDBM50377352 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_479558 (CHEMBL929422) |
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IC50 | 53±n/a nM |
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Citation | Ruel, R; Thibeault, C; L'Heureux, A; Martel, A; Cai, ZW; Wei, D; Qian, L; Barrish, JC; Mathur, A; D'Arienzo, C; Hunt, JT; Kamath, A; Marathe, P; Zhang, Y; Derbin, G; Wautlet, B; Mortillo, S; Jeyaseelan, R; Henley, B; Tejwani, R; Bhide, RS; Trainor, GL; Fargnoli, J; Lombardo, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Vascular endothelial growth factor receptor 2 |
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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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BDBM50377352 |
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n/a |
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Name | BDBM50377352 |
Synonyms: | BMS-645737 | CHEMBL261592 |
Type | Small organic molecule |
Emp. Form. | C20H20N8O |
Mol. Mass. | 388.4258 |
SMILES | CC(C)c1c(cn2ncnc(Nc3cnc4[nH]c(C)cc4c3)c12)-c1nnc(C)o1 |
Structure |
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