Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM14995
Substrate
Gastrin Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
46±n/a nM
Citation
 Hodous, BL; Geuns-Meyer, SD; Hughes, PE; Albrecht, BK; Bellon, S; Bready, J; Caenepeel, S; Cee, VJ; Chaffee, SC; Coxon, A; Emery, M; Fretland, J; Gallant, P; Gu, Y; Hoffman, D; Johnson, RE; Kendall, R; Kim, JL; Long, AM; Morrison, M; Olivieri, PR; Patel, VF; Polverino, A; Rose, P; Tempest, P; Wang, L; Whittington, DA; Zhao, H Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem 50:611-26 (2007) [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:
BDBM14995
Synonyms:
2-(Methylamino)pyrimidine 58 | N-(2-((3-(Dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)-phenyl)-2-fluoro-5-(3-(2-(methylamino)pyrimidin-4-yl)pyridin-2-yloxy)benzamide | N-(2-{[3-(dimethylamino)propyl](methyl)amino}-5-(trifluoromethyl)phenyl)-2-fluoro-5-({3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl}oxy)benzamide
Type:
Small organic molecule
Emp. Form.:
C30H31F4N7O2
Mol. Mass.:
597.6065
SMILES:
CNc1nccc(n1)-c1cccnc1Oc1ccc(F)c(c1)C(=O)Nc1cc(ccc1N(C)CCCN(C)C)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Gastrin Peptide Substrate
Synonyms:
Biotinylated gastrin peptide substrate | biotinylated gastrin substrate | gastrin substrate
Type:
Peptide
Mol. Mass.:
1823.88
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINEEEEAYGWLDF