| Reaction Details |
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 | Report a problem with these data |
| Target | Vascular endothelial growth factor receptor 1 |
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| Ligand | BDBM50181320 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_347371 (CHEMBL865651) |
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| IC50 | 10±n/a nM |
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| Citation |  Frazier, K; Jazan, E; McBride, CM; Pecchi, S; Renhowe, PA; Shafer, CM; Taylor, C; Bussiere, D; He, MM; Jansen, JM; Lapointe, G; Ma, S; Vora, J; Wiesmann, M Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett16:2247-51 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, 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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| BDBM50181320 |
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| n/a |
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| Name | BDBM50181320 |
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| Synonyms: | 4-Amino-3-[6-(4-methylpiperazinyl)benzimidazol-2-yl]hydroquinolin-2-one | 4-amino-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-onecn | CHEMBL204427 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H22N6O |
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| Mol. Mass. | 374.439 |
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| SMILES | CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1c(N)c2ccccc2[nH]c1=O |
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| Structure | 
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