| Reaction Details |
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 | Report a problem with these data |
| Target | Vascular endothelial growth factor receptor 1 |
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| Ligand | BDBM50188748 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_390502 (CHEMBL869848) |
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| IC50 | 863±n/a nM |
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| Citation |  Dinges, J; Ashworth, KL; Akritopoulou-Zanze, I; Akritopolou-Zanze, I; Arnold, LD; Baumeister, SA; Bousquet, PF; Cunha, GA; Davidsen, SK; Djuric, SW; Gracias, VJ; Michaelides, MR; Rafferty, P; Sowin, TJ; Stewart, KD; Xia, Z; Zhang, HQ 1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett16:4266-71 (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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| BDBM50188748 |
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| n/a |
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| Name | BDBM50188748 |
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| Synonyms: | 1-((5-(6-((4-methylpiperazin-1-yl)methyl)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)thiophen-2-yl)methyl)-3-(3-(trifluoromethyl)phenyl)urea | CHEMBL212986 |
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| Type | Small organic molecule |
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| Emp. Form. | C29H29F3N6OS |
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| Mol. Mass. | 566.64 |
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| SMILES | CN1CCN(Cc2ccc-3c(Cc4c-3n[nH]c4-c3ccc(CNC(=O)Nc4cccc(c4)C(F)(F)F)s3)c2)CC1 |
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| Structure | 
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