Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM5408
Substrate
poly-Glu/Tyr
Meas. Tech.
Kinase Inhibition Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
232±n/a nM
Citation
 Fraley, ME; Rubino, RS; Hoffman, WF; Hambaugh, SR; Arrington, KL; Hungate, RW; Bilodeau, MT; Tebben, AJ; Rutledge, RZ; Kendall, RL; McFall, RC; Huckle, WR; Coll, KE; Thomas, KA Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. Bioorg Med Chem Lett 12:3537-41 (2002) [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:
BDBM5408
Synonyms:
1-{2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl}-1H-imidazole-2-carbonitrile | 2,4-Disubstituted Pyrimidine 5j
Type:
Small organic molecule
Emp. Form.:
C16H14N6
Mol. Mass.:
290.3226
SMILES:
Cc1cc(C)cc(Nc2nccc(n2)-n2ccnc2C#N)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly-Glu/Tyr
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
poly-Glu/Tyr (4:1). 25 uM ATP/10 uCi [gamma-33P]ATP as co-substrate.
Residue:
3
Sequence:
NA