| Reaction Details |
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 | Report a problem with these data |
| Target | Vascular endothelial growth factor receptor 1 |
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| Ligand | BDBM24773 |
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| Substrate/Competitor | biotinylated gastrin substrate |
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| Meas. Tech. | HTRF Kinase Inhibition Assay |
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| pH | 7.5±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 2±0.7 nM |
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| Citation |  Polverino, A; Coxon, A; Starnes, C; Diaz, Z; DeMelfi, T; Wang, L; Bready, J; Estrada, J; Cattley, R; Kaufman, S; Chen, D; Gan, Y; Kumar, G; Meyer, J; Neervannan, S; Alva, G; Talvenheimo, J; Montestruque, S; Tasker, A; Patel, V; Radinsky, R; Kendall, R AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res66:8715-21 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Vascular endothelial growth factor receptor 1 |
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| Name: | Vascular endothelial growth factor receptor 1 |
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| 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 |
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| Type: | Receptor Tyrosine Kinase |
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| Mol. Mass.: | 150800.23 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P17948 |
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| Residue: | 1338 |
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| Sequence: | MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET
ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD
GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV
KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK
MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK
AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA
TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC
DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK
VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM
HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA
PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER
VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI
RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK
VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK
QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV
TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH
RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS
DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD
PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA
PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW
TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC
CSPPPDYNSVVLYSTPPI
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| BDBM24773 |
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| biotinylated gastrin substrate |
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| Name: | biotinylated gastrin substrate |
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| Synonyms: | n/a |
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| Type: | Peptide |
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| Mol. Mass.: | 2100.22 |
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| Organism: | n/a |
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| Description: | n/a |
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| Residue: | 17 |
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| Sequence: | |
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