Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM6398
Substrate
Biotinylated VEGF-R Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
135±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:
BDBM6398
Synonyms:
N-(3-chlorophenyl)-6-(5-{[3-(dimethylamino)propyl]amino}pyridin-3-yl)pyrazin-2-amine | N-{5-[6-(3-Chloro-phenylamino)-pyrazin-2-yl]-pyridin-3-yl}-N ,N -dimethyl-propane-1,3-diamine | Pyrazine-Pyridine Biheteroaryl 40
Type:
Small organic molecule
Emp. Form.:
C20H23ClN6
Mol. Mass.:
382.89
SMILES:
CN(C)CCCNc1cncc(c1)-c1cncc(Nc2cccc(Cl)c2)n1
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