Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM12320
Substrate
Biotinylated VEGF-R Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
8±n/a
Temperature
303.15±n/a K
IC50
146±n/a nM
Citation
Huang, S; Li, R; Connolly, PJ; Xu, G; Gaul, MD; Emanuel, SL; Lamontagne, KR; Greenberger, LM Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors. Bioorg Med Chem Lett 16:6063-6 (2006) [PubMed] Article
More Info.:
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:
BDBM12320
Synonyms:
5-[(1E)-(methoxyimino)methyl]-6-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-4-amine | oxime analog 9
Type:
Small organic molecule
Emp. Form.:
C15H15N5O2
Mol. Mass.:
297.3119
SMILES:
CO\N=C\c1c(N)ncnc1Oc1ccc2[nH]c(C)cc2c1
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