Reaction Details |
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Target | Polycomb protein EED |
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Ligand | BDBM223987 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Radioligand Binding Assay |
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Temperature | 296.15±0 K |
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IC50 | 18±2 nM |
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Citation | He, Y; Selvaraju, S; Curtin, ML; Jakob, CG; Zhu, H; Comess, KM; Shaw, B; The, J; Lima-Fernandes, E; Szewczyk, MM; Cheng, D; Klinge, KL; Li, HQ; Pliushchev, M; Algire, MA; Maag, D; Guo, J; Dietrich, J; Panchal, SC; Petros, AM; Sweis, RF; Torrent, M; Bigelow, LJ; Senisterra, G; Li, F; Kennedy, S; Wu, Q; Osterling, DJ; Lindley, DJ; Gao, W; Galasinski, S; Barsyte-Lovejoy, D; Vedadi, M; Buchanan, FG; Arrowsmith, CH; Chiang, GG; Sun, C; Pappano, WN The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat Chem Biol13:389-395 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Polycomb protein EED |
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Name: | Polycomb protein EED |
Synonyms: | EED | EED_HUMAN | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1 | hEED |
Type: | Protein |
Mol. Mass.: | 50201.68 |
Organism: | Homo sapiens (Human) |
Description: | O75530 |
Residue: | 441 |
Sequence: | MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTP
NAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNR
VTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITM
QCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVL
SADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFS
TRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQ
CDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSR
DSSILIAVCDDASIWRWDRLR
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BDBM223987 |
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n/a |
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Name | BDBM223987 |
Synonyms: | A-395 (5) | rac-(3R,4S)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-4-(4-(4-(methylsulfonyl)piperazin-1-yl)phenyl)pyrrolidin-3-amine (4) |
Type | Small organic molecule |
Emp. Form. | C26H35FN4O2S |
Mol. Mass. | 486.645 |
SMILES | CN(C)[C@H]1CN(C[C@@H]1c1ccc(cc1)N1CCN(CC1)S(C)(=O)=O)C1CCc2cccc(F)c12 |r,w:24.26| |
Structure |
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