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Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM6428
Substrate
Biotinylated VEGF-R Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
>10000±n/a nM
Citation
 Kuo, GH; Wang, A; Emanuel, S; Deangelis, A; Zhang, R; Connolly, PJ; Murray, WV; Gruninger, RH; Sechler, J; Fuentes-Pesquera, A; Johnson, D; Middleton, SA; Jolliffe, L; Chen, X Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem 48:1886-900 (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:
BDBM6428
Synonyms:
3-[(5-{5-[(3-chlorophenyl)amino]pyrazin-2-yl}pyridin-3-yl)amino]propan-1-ol | 3-[[5-[5-[(3-chlorophenyl)amino]pyrazinyl]-3-pyridinyl]amino]-1-propanol | Pyrazine-Pyridine deriv. 20
Type:
Small organic molecule
Emp. Form.:
C18H18ClN5O
Mol. Mass.:
355.821
SMILES:
OCCCNc1cncc(c1)-c1cnc(Nc2cccc(Cl)c2)cn1
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