Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM4630
Substrate
poly(E,A,Y)
Meas. Tech.
VEGF-R Kinase Inhibition Assay
Temperature
298.15±n/a K
IC50
<2±n/a nM
Comments
extracted
Citation
 Hennequin, LFThomas, APJohnstone, CStokes, ESPlé, PALohmann, JJOgilvie, DJDukes, MWedge, SRCurwen, JOKendrew, JLambert-van der Brempt, C Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. J Med Chem 42:5369-89 (1999) [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:
BDBM4630
Synonyms:
2-chloro-4-fluoro-5-{[6-methoxy-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenol | Anilinoquinazoline deriv. 13 | N-(4-Chloro-2-fluoro-5-hydroxyphenyl)-6-methoxy-7-(2-methoxyethoxy)-4-quinazolinylamine
Type:
Small organic molecule
Emp. Form.:
C18H17ClFN3O4
Mol. Mass.:
393.797
SMILES:
COCCOc1cc2ncnc(Nc3cc(O)c(Cl)cc3F)c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(E,A,Y)
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
A poly(glu, ala, tyr) 6:3:1 random copolymer. 2 uM ATP was used as co-substrate.
Residue:
3
Sequence:
NA