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Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM6421
Substrate
Biotinylated VEGF-R Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
67±n/a nM
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 Chem 48:4892-909 (2005) [PubMed]  Article 
Target
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:
MESRALLAVALWFCVETRAASVGLPGDSLHPPKLSTQKDILTILANTTLQITCRGQRDLDWLWPNTPRDSEERVLVTECGDSIFCKTLTVPRVVGNDTGAYKCFYRDTDVSSIVYVYVQDHRSPFIASVSDEHGIVYITENKNKTVVIPCRGSISNLNVSLCARYPEKRFVPDGNRISWDSEKGFTIPSYMISYAGMVFCEAKINDETYQSIMYIVLVVGYRIYDVVLSPPHEIELSAGEKLVLNCTARTELNVGLDFSWQFPSSKHQHKKIVNRDVKSLPGTVAKMFLSTLTIDSVTKSDQGEYTCTAYSGLMTKKNKTFVRVHTKPFIAFGSGMKSLVEATVGSQVRIPVKYLSYPAPDIKWYRNGRPIESNYTMIVGDELTIMEVSERDAGNYTVILTNPISMEKQSHMVSLVVNVPPQIGEKALISPMDSYQYGTMQTLTCTVYANPPLHHIQWYWQLEEACSYRPSQTNPYTCKEWRHVKDFQGGNKIEVTKNQYALIEGKNKTVSTLVIQAAYVSALYKCEAINKAGRGERVISFHVIRGPEITVQPATQPTERESMSLLCTADRNTFENLTWYKLGSQATSVHMGESLTPVCKNLDALWKLNGTVFSNSTNDILIVAFQNASLQDQGNYVCSAQDKKTKKRHCLVKQLVILERMAPMITGNLENQTTTIGETIEVVCPTSGNPTPLITWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDGGLYTCQACNVLGCARAETLFIIEGVQEKTNLEVIILVGTAVIAMFFWLLLVILVRTVKRANEGELKTGYLSIVMDPDELPLDERCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCKTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRGKRNEFVPYKSKGARFRSGKDYVGELSVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEASEELYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDPRLPLKWMAPETIFDRIYTIQSGVWSFGVLLWEIFSLGASPYPGVKIDEKFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHEDPNQRPAFSELVEHLGNLLQANAQQDGKDYIVLPMSETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISHYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDSQTDSGMVLASEELKTLEDRNKLSPSFGGMMPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSDEAGLLKLVDVAGHVDSGTTLRSSPV
  
Inhibitor
Name:
BDBM6421
Synonyms:
N-(3-Chlorophenyl)-6-[5-[[3-(1H-1,2,4-triazol-1-yl)propyl]amino]-3-pyridinyl]-2-pyrazinamine | N-(3-chlorophenyl)-6-(5-{[3-(1H-1,2,4-triazol-1-yl)propyl]amino}pyridin-3-yl)pyrazin-2-amine | Pyrazine-Pyridine Biheteroaryl 58
Type:
Small organic molecule
Emp. Form.:
C20H19ClN8
Mol. Mass.:
406.871
SMILES:
Clc1cccc(Nc2cncc(n2)-c2cncc(NCCCn3cncn3)c2)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated VEGF-R Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2588.40
Organism:
n/a
Description:
n/a
Residue:
23
Sequence:
ITINKHKKLAEGSAYEEVAMIDE