Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM21098
Substrate
biotinylated peptide substrate
Meas. Tech.
HTRF Assay of Receptor Tyrosine Kinase and Cellular KDR Phosphorylation Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
23±n/a nM
EC50
94±n/a nM
Citation
 Ji, ZAhmed, AAAlbert, DHBouska, JJBousquet, PFCunha, GADiaz, GGlaser, KBGuo, JHarris, CMLi, JMarcotte, PAMoskey, MDOie, TPease, LSoni, NBStewart, KDDavidsen, SKMichaelides, MR 3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases. J Med Chem 51:1231-41 (2008) [PubMed]  Article 
Target
Name:
Vascular endothelial growth factor receptor 2
Synonyms:
CD_antigen=CD309 | FLK1 | Fetal liver kinase 1 (FLK-1) | Flk-1/KDR | KDR | Kinase Insert Domain Receptor | Protein-tyrosine kinase receptor Flk-1 | VEGFR kinase (KDR) | VEGFR-2 | VEGFR-2 (KDR) | VEGFR2 | VGFR2_HUMAN | Vascular Endothelial Growth Factor Receptor Kinase 2 | Vascular endothelial growth factor receptor (VEGFR-2) | Vascular endothelial growth factor receptor 2 (KDR) | Vascular endothelial growth factor receptor 2 (VEGFR-2) | Vascular endothelial growth factor receptor 2 (VEGFR2) | Vascular endothelial growth factor receptor 2 precursor (VEGFR-2) | Vascular endothelial growth factor receptor-2 (VEGFR-2)
Type:
Receptor Tyrosine Kinase
Mol. Mass.:
151510.97
Organism:
Homo sapiens (Human)
Description:
P35968
Residue:
1356
Sequence:
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
  
Inhibitor
Name:
BDBM21098
Synonyms:
3-[4-(3-amino-1,2-benzoxazol-4-yl)phenyl]-1-[4-fluoro-3-(trifluoromethyl)phenyl]urea | Aminobenzoisoxazole, 41
Type:
Small organic molecule
Emp. Form.:
C21H14F4N4O2
Mol. Mass.:
430.3551
SMILES:
Nc1noc2cccc(-c3ccc(NC(=O)Nc4ccc(F)c(c4)C(F)(F)F)cc3)c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2470.20
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ITINAHAEEEYFFLFAAMIDE