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TargetPolycomb protein EED
LigandBDBM223987
Substrate/Competitorn/a
Meas. Tech.Radioligand Binding Assay
Temperature296.15±0 K
IC50 18±2 nM
Citation He, YSelvaraju, SCurtin, MLJakob, CGZhu, HComess, KMShaw, BThe, JLima-Fernandes, ESzewczyk, MMCheng, DKlinge, KLLi, HQPliushchev, MAlgire, MAMaag, DGuo, JDietrich, JPanchal, SCPetros, AMSweis, RFTorrent, MBigelow, LJSenisterra, GLi, FKennedy, SWu, QOsterling, DJLindley, DJGao, WGalasinski, SBarsyte-Lovejoy, DVedadi, MBuchanan, FGArrowsmith, CHChiang, GGSun, CPappano, WN The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat Chem Biol13:389-395 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Polycomb protein EED
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM223987
n/a
NameBDBM223987
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)
TypeSmall organic molecule
Emp. Form.C26H35FN4O2S
Mol. Mass.486.645
SMILESCN(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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