Reaction Details |
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Target | Angiopoietin-1 receptor |
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Ligand | BDBM50318963 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_635311 (CHEMBL1119624) |
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IC50 | 3±n/a nM |
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Citation | Hudkins, RL; Zulli, AL; Underiner, TL; Angeles, TS; Aimone, LD; Meyer, SL; Pauletti, D; Chang, H; Fedorov, EV; Almo, SC; Fedorov, AA; Ruggeri, BA 8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett20:3356-60 (2010) [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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BDBM50318963 |
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n/a |
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Name | BDBM50318963 |
Synonyms: | CHEMBL1084061 | rac-5-methyl-9-propyl-12-(tetrahydro-2H-pyran-2-yl)-5,7,8,9-tetrahydro-1H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-3(2H)-one |
Type | Small organic molecule |
Emp. Form. | C28H30N4O2 |
Mol. Mass. | 454.5634 |
SMILES | CCCn1c2ccc(cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12)C1CCCCO1 |
Structure |
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