Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM24505
Substrate
poly(Glu4, Tyr)
Meas. Tech.
In Vitro Kinase Assay
IC50
17±n/a nM
Citation
 Claridge, SRaeppel, FGranger, MCBernstein, NSaavedra, OZhan, LLlewellyn, DWahhab, ADeziel, RRahil, JBeaulieu, NNguyen, HDupont, IBarsalou, ABeaulieu, CChute, IGravel, SRobert, MFLefebvre, SDubay, MPascal, RGillespie, JJin, ZWang, JBesterman, JMMacLeod, ARVaisburg, A Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett 18:2793-8 (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:
BDBM24505
Synonyms:
3-(3-fluoro-4-{[2-(pyridin-2-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-1-(2-phenylacetyl)thiourea | thieno[3,2-b]pyridine-based inhibitor, 10h
Type:
Small organic molecule
Emp. Form.:
C27H19FN4O2S2
Mol. Mass.:
514.594
SMILES:
Fc1cc(NC(=S)NC(=O)Cc2ccccc2)ccc1Oc1ccnc2cc(sc12)-c1ccccn1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(Glu4, Tyr)
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA