| Reaction Details |
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 | Report a problem with these data |
| Target | Angiopoietin-1 receptor |
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| Ligand | BDBM14974 |
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| Substrate/Competitor | Her2 Peptide Substrate |
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| Meas. Tech. | Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme 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 | 1±n/a nM |
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| Citation |  Hodous, BL; Geuns-Meyer, SD; Hughes, PE; Albrecht, BK; Bellon, S; Bready, J; Caenepeel, S; Cee, VJ; Chaffee, SC; Coxon, A; Emery, M; Fretland, J; Gallant, P; Gu, Y; Hoffman, D; Johnson, RE; Kendall, R; Kim, JL; Long, AM; Morrison, M; Olivieri, PR; Patel, VF; Polverino, A; Rose, P; Tempest, P; Wang, L; Whittington, DA; Zhao, H Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem50:611-26 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Angiopoietin-1 receptor |
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| Name: | Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2) |
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| Synonyms: | Tyrosine-protein kinase TIE-2 | Tyrosine-protein kinase receptor (TIE-2) | Tyrosine-protein kinase receptor TEK | Tyrosine-protein kinase receptor TEK (p140 TEK) | Tyrosine-protein kinase receptor TIE-2 | Tyrosine-protein kinase receptor TIE2/TEK | p140 TEK |
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| Type: | Enzyme |
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| Mol. Mass.: | 125835.70 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q02763 |
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| Residue: | 1124 |
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| Sequence: | MDSLASLVLCGVSLLLSGTVEGAMDLILINSLPLVSDAETSLTCIASGWRPHEPITIGRD
FEALMNQHQDPLEVTQDVTREWAKKVVWKREKASKINGAYFCEGRVRGEAIRIRTMKMRQ
QASFLPATLTMTVDKGDNVNISFKKVLIKEEDAVIYKNGSFIHSVPRHEVPDILEVHLPH
AQPQDAGVYSARYIGGNLFTSAFTRLIVRRCEAQKWGPECNHLCTACMNNGVCHEDTGEC
ICPPGFMGRTCEKACELHTFGRTCKERCSGQEGCKSYVFCLPDPYGCSCATGWKGLQCNE
ACHPGFYGPDCKLRCSCNNGEMCDRFQGCLCSPGWQGLQCEREGIQRMTPKIVDLPDHIE
VNSGKFNPICKASGWPLPTNEEMTLVKPDGTVLHPKDFNHTDHFSVAIFTIHRILPPDSG
VWVCSVNTVAGMVEKPFNISVKVLPKPLNAPNVIDTGHNFAVINISSEPYFGDGPIKSKK
LLYKPVNHYEAWQHIQVTNEIVTLNYLEPRTEYELCVQLVRRGEGGEGHPGPVRRFTTAS
IGLPPPRGLNLLPKSQTTLNLTWQPIFPSSEDDFYVEVERRSVQKSDQQNIKVPGNLTSV
LLNNLHPREQYVVRARVNTKAQGEWSEDLTAWTLSDILPPQPENIKISNITHSSAVISWT
ILDGYSISSITIRYKVQGKNEDQHVDVKIKNATITQYQLKGLEPETAYQVDIFAENNIGS
SNPAFSHELVTLPESQAPADLGGGKMLLIAILGSAGMTCLTVLLAFLIILQLKRANVQRR
MAQAFQNVREEPAVQFNSGTLALNRKVKNNPDPTIYPVLDWNDIKFQDVIGEGNFGQVLK
ARIKKDGLRMDAAIKRMKEYASKDDHRDFAGELEVLCKLGHHPNIINLLGACEHRGYLYL
AIEYAPHGNLLDFLRKSRVLETDPAFAIANSTASTLSSQQLLHFAADVARGMDYLSQKQF
IHRDLAARNILVGENYVAKIADFGLSRGQEVYVKKTMGRLPVRWMAIESLNYSVYTTNSD
VWSYGVLLWEIVSLGGTPYCGMTCAELYEKLPQGYRLEKPLNCDDEVYDLMRQCWREKPY
ERPSFAQILVSLNRMLEERKTYVNTTLYEKFTYAGIDCSAEEAA
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| BDBM14974 |
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| Name | BDBM14974 |
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| Synonyms: | CHEMBL221484 | N-(3-(3-(Dimethylamino)propyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(3-(pyrimidin-4-yl)pyridin-2-ylamino)benzamide | N-{3-[3-(dimethylamino)propyl]-5-(trifluoromethyl)phenyl}-4-methyl-3-{[3-(pyrimidin-4-yl)pyridin-2-yl]amino}benzamide | pyridinyl pyrimidine 39 |
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| Type | Small organic molecule |
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| Emp. Form. | C29H29F3N6O |
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| Mol. Mass. | 534.5754 |
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| SMILES | CN(C)CCCc1cc(NC(=O)c2ccc(C)c(Nc3ncccc3-c3ccncn3)c2)cc(c1)C(F)(F)F |
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| Structure |  |
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| Her2 Peptide Substrate |
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| Name: | Her2 Peptide Substrate |
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| Synonyms: | Biotinylated Her2 Peptide Substrate | biotinylated long chain peptide |
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| Type: | Peptide |
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| Mol. Mass.: | 2278.65 |
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| Organism: | n/a |
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| Description: | n/a |
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| Residue: | 20 |
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| Sequence: | |
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