Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM14971
Substrate
Gastrin Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
4±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
More Info.:
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:
Human
Description:
P35968
Residue:
1356
Sequence:
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
Inhibitor
Name:
BDBM14971
Synonyms:
4-Methyl-3-(3-(pyrimidin-4-yl)pyridin-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide | 4-methyl-3-{[3-(pyrimidin-4-yl)pyridin-2-yl]amino}-N-[3-(trifluoromethyl)phenyl]benzamide | JMC526189 Compound 2 | pyridinyl pyrimidine 6
Type:
Small organic molecule
Emp. Form.:
C24H18F3N5O
Mol. Mass.:
449.4278
SMILES:
Cc1ccc(cc1Nc1ncccc1-c1ccncn1)C(=O)Nc1cccc(c1)C(F)(F)F
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