Reaction Details |
| Report a problem with these data |
Target | Vascular endothelial growth factor receptor 1 |
---|
Ligand | BDBM4877 |
---|
Substrate/Competitor | polyGluTyr |
---|
Meas. Tech. | Kinase Inhibition Assay |
---|
IC50 | 260±n/a nM |
---|
Citation | Bold, G; Altmann, KH; Frei, J; Lang, M; Manley, PW; Traxler, P; Wietfeld, B; Bruggen, J; Buchdunger, E; Cozens, R; Ferrari, S; Furet, P; Hofmann, F; Martiny-Baron, G; Mestan, J; Rosel, J; Sills, M; Stover, D; Acemoglu, F; Boss, E; Emmenegger, R; Lasser, L; Masso, E; Roth, R; Schlachter, C; Vetterli, W New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J Med Chem43:2310-23 (2000) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Vascular endothelial growth factor receptor 1 |
---|
Name: | Vascular endothelial growth factor receptor 1 |
Synonyms: | FLT | FLT1 | FRT | Flt-1 | Fms-like tyrosine kinase 1 | Platelet-derived growth factor receptor beta (PDGFRB) | Tyrosine-protein kinase FRT | Tyrosine-protein kinase receptor FLT | VEGFR-1 | VEGFR1 | VGFR1_HUMAN | Vascular endothelial growth factor receptor (VEGFR) | Vascular endothelial growth factor receptor 1 (FLT1) | Vascular endothelial growth factor receptor 1 (VEGFR1) | Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) | Vascular endothelial growth factor receptor 1 precursor | Vascular permeability factor receptor | fms-related tyrosine kinase 1 | vascular endothelial growth factor/vascular permeability factor receptor |
Type: | Receptor Tyrosine Kinase |
Mol. Mass.: | 150800.23 |
Organism: | Homo sapiens (Human) |
Description: | P17948 |
Residue: | 1338 |
Sequence: | MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET
ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD
GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV
KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK
MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK
AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA
TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC
DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK
VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM
HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA
PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER
VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI
RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK
VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK
QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV
TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH
RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS
DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD
PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA
PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW
TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC
CSPPPDYNSVVLYSTPPI
|
|
|
BDBM4877 |
---|
polyGluTyr |
---|
Name: | polyGluTyr |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | polyGluTyr(4:1).
8 uM ATP and 0.2 uCi [gamma-33P]ATP as co-substrate. |
Residue: | 3 |
Sequence: | |