Reaction Details |
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Target | Vascular endothelial growth factor receptor 2 |
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Ligand | BDBM50184807 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_342121 (CHEMBL859792) |
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Ki | 28±n/a nM |
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Citation | Bhide, RS; Cai, ZW; Zhang, YZ; Qian, L; Wei, D; Barbosa, S; Lombardo, LJ; Borzilleri, RM; Zheng, X; Wu, LI; Barrish, JC; Kim, SH; Leavitt, K; Mathur, A; Leith, L; Chao, S; Wautlet, B; Mortillo, S; Jeyaseelan, R; Kukral, D; Hunt, JT; Kamath, A; Fura, A; Vyas, V; Marathe, P; D'Arienzo, C; Derbin, G; Fargnoli, J 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. J Med Chem49:2143-6 (2006) [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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BDBM50184807 |
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n/a |
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Name | BDBM50184807 |
Synonyms: | (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol | (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 | CHEMBL377300 |
Type | Small organic molecule |
Emp. Form. | C19H19FN4O3 |
Mol. Mass. | 370.3776 |
SMILES | C[C@@H](O)COc1cn2ncnc(Oc3ccc4[nH]c(C)cc4c3F)c2c1C |
Structure |
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