Reaction Details |
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Target | Vascular endothelial growth factor receptor 2 |
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Ligand | BDBM6420 |
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Substrate/Competitor | Biotinylated VEGF-R Peptide Substrate |
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Meas. Tech. | Kinase Inhibition Assay |
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IC50 | 94±n/a nM |
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Citation | Kuo, GH; Prouty, C; Wang, A; Emanuel, S; Deangelis, A; Zhang, Y; Song, F; Beall, L; Connolly, PJ; Karnachi, P; Chen, X; Gruninger, RH; Sechler, J; Fuentes-Pesquera, A; Middleton, SA; Jolliffe, L; Murray, WV Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors. J Med Chem48:4892-909 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Vascular endothelial growth factor receptor 2 |
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Name: | Vascular endothelial growth factor receptor 2 |
Synonyms: | Fetal liver kinase 1 | Flk1 | Kdr | VEGFR-2 (KDR) | VGFR2_RAT |
Type: | Receptor Tyrosine Kinase |
Mol. Mass.: | 150388.56 |
Organism: | Rattus norvegicus (rat) |
Description: | VEGF-R is a fusion protein containing a polyhistidine tag at the N-terminus followed by amino acids 786-1343 of the rat VEGF-R2 kinase domain. |
Residue: | 1343 |
Sequence: | MESRALLAVALWFCVETRAASVGLPGDSLHPPKLSTQKDILTILANTTLQITCRGQRDLD
WLWPNTPRDSEERVLVTECGDSIFCKTLTVPRVVGNDTGAYKCFYRDTDVSSIVYVYVQD
HRSPFIASVSDEHGIVYITENKNKTVVIPCRGSISNLNVSLCARYPEKRFVPDGNRISWD
SEKGFTIPSYMISYAGMVFCEAKINDETYQSIMYIVLVVGYRIYDVVLSPPHEIELSAGE
KLVLNCTARTELNVGLDFSWQFPSSKHQHKKIVNRDVKSLPGTVAKMFLSTLTIDSVTKS
DQGEYTCTAYSGLMTKKNKTFVRVHTKPFIAFGSGMKSLVEATVGSQVRIPVKYLSYPAP
DIKWYRNGRPIESNYTMIVGDELTIMEVSERDAGNYTVILTNPISMEKQSHMVSLVVNVP
PQIGEKALISPMDSYQYGTMQTLTCTVYANPPLHHIQWYWQLEEACSYRPSQTNPYTCKE
WRHVKDFQGGNKIEVTKNQYALIEGKNKTVSTLVIQAAYVSALYKCEAINKAGRGERVIS
FHVIRGPEITVQPATQPTERESMSLLCTADRNTFENLTWYKLGSQATSVHMGESLTPVCK
NLDALWKLNGTVFSNSTNDILIVAFQNASLQDQGNYVCSAQDKKTKKRHCLVKQLVILER
MAPMITGNLENQTTTIGETIEVVCPTSGNPTPLITWFKDNETLVEDSGIVLKDGNRNLTI
RRVRKEDGGLYTCQACNVLGCARAETLFIIEGVQEKTNLEVIILVGTAVIAMFFWLLLVI
LVRTVKRANEGELKTGYLSIVMDPDELPLDERCERLPYDASKWEFPRDRLKLGKPLGRGA
FGQVIEADAFGIDKTATCKTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGA
CTKPGGPLMVIVEFCKFGNLSTYLRGKRNEFVPYKSKGARFRSGKDYVGELSVDLKRRLD
SITSSQSSASSGFVEEKSLSDVEEEEASEELYKDFLTLEHLICYSFQVAKGMEFLASRKC
IHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDPRLPLKWMAPETIFDRIYTI
QSGVWSFGVLLWEIFSLGASPYPGVKIDEKFCRRLKEGTRMRAPDYTTPEMYQTMLDCWH
EDPNQRPAFSELVEHLGNLLQANAQQDGKDYIVLPMSETLSMEEDSGLSLPTSPVSCMEE
EEVCDPKFHYDNTAGISHYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDSQTDSGMVL
ASEELKTLEDRNKLSPSFGGMMPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSDEA
GLLKLVDVAGHVDSGTTLRSSPV
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BDBM6420 |
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Biotinylated VEGF-R Peptide Substrate |
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Name: | Biotinylated VEGF-R Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2588.40 |
Organism: | n/a |
Description: | n/a |
Residue: | 23 |
Sequence: | (Biotin)KHKKLAEGSAYEEV-Amide
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