Reaction Details |
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Target | Angiopoietin-1 receptor |
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Ligand | BDBM50272587 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_510306 (CHEMBL995225) |
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IC50 | 13000±n/a nM |
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Citation | Buttar, D; Edge, M; Emery, SC; Fitzek, M; Forder, C; Griffen, A; Hayter, B; Hayward, CF; Hopcroft, PJ; Luke, RW; Page, K; Stawpert, J; Wright, A Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable. Bioorg Med Chem Lett18:4723-6 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Angiopoietin-1 receptor |
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Name: | Angiopoietin-1 receptor |
Synonyms: | TEK | TIE2 | TIE2_HUMAN | 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 | VMCM | VMCM1 | Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2) | p140 TEK |
Type: | Enzyme |
Mol. Mass.: | 125835.70 |
Organism: | Homo sapiens (Human) |
Description: | Q02763 |
Residue: | 1124 |
Sequence: | MDSLASLVLCGVSLLLSGTVEGAMDLILINSLPLVSDAETSLTCIASGWRPHEPITIGRD
FEALMNQHQDPLEVTQDVTREWAKKVVWKREKASKINGAYFCEGRVRGEAIRIRTMKMRQ
QASFLPATLTMTVDKGDNVNISFKKVLIKEEDAVIYKNGSFIHSVPRHEVPDILEVHLPH
AQPQDAGVYSARYIGGNLFTSAFTRLIVRRCEAQKWGPECNHLCTACMNNGVCHEDTGEC
ICPPGFMGRTCEKACELHTFGRTCKERCSGQEGCKSYVFCLPDPYGCSCATGWKGLQCNE
ACHPGFYGPDCKLRCSCNNGEMCDRFQGCLCSPGWQGLQCEREGIQRMTPKIVDLPDHIE
VNSGKFNPICKASGWPLPTNEEMTLVKPDGTVLHPKDFNHTDHFSVAIFTIHRILPPDSG
VWVCSVNTVAGMVEKPFNISVKVLPKPLNAPNVIDTGHNFAVINISSEPYFGDGPIKSKK
LLYKPVNHYEAWQHIQVTNEIVTLNYLEPRTEYELCVQLVRRGEGGEGHPGPVRRFTTAS
IGLPPPRGLNLLPKSQTTLNLTWQPIFPSSEDDFYVEVERRSVQKSDQQNIKVPGNLTSV
LLNNLHPREQYVVRARVNTKAQGEWSEDLTAWTLSDILPPQPENIKISNITHSSAVISWT
ILDGYSISSITIRYKVQGKNEDQHVDVKIKNATITQYQLKGLEPETAYQVDIFAENNIGS
SNPAFSHELVTLPESQAPADLGGGKMLLIAILGSAGMTCLTVLLAFLIILQLKRANVQRR
MAQAFQNVREEPAVQFNSGTLALNRKVKNNPDPTIYPVLDWNDIKFQDVIGEGNFGQVLK
ARIKKDGLRMDAAIKRMKEYASKDDHRDFAGELEVLCKLGHHPNIINLLGACEHRGYLYL
AIEYAPHGNLLDFLRKSRVLETDPAFAIANSTASTLSSQQLLHFAADVARGMDYLSQKQF
IHRDLAARNILVGENYVAKIADFGLSRGQEVYVKKTMGRLPVRWMAIESLNYSVYTTNSD
VWSYGVLLWEIVSLGGTPYCGMTCAELYEKLPQGYRLEKPLNCDDEVYDLMRQCWREKPY
ERPSFAQILVSLNRMLEERKTYVNTTLYEKFTYAGIDCSAEEAA
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BDBM50272587 |
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n/a |
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Name | BDBM50272587 |
Synonyms: | (E/Z)-4-(2-(6-(p-fluoro-phenyl)imidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine | CHEMBL524799 |
Type | Small organic molecule |
Emp. Form. | C17H12FN5S |
Mol. Mass. | 337.374 |
SMILES | Nc1nccc(\C=C\c2c(nc3sccn23)-c2ccc(F)cc2)n1 |
Structure |
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