Reaction Details
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Polycomb protein EED
Ligand
BDBM223985
Substrate
n/a
Meas. Tech.
TR-FRET Binding Assay
pH
7.5±0
Temperature
298.15±0 K
Ki
4±0.0 nM
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 Biol 13:389-395 (2017) [PubMed] Article More Info.:
Target
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:
MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
Inhibitor
Name:
BDBM223985
Synonyms:
rac-(3R,4S)-1-(2-fluoro-6-methylbenzyl)-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine (2)
Type:
Small organic molecule
Emp. Form.:
C23H28FN3
Mol. Mass.:
365.4869
SMILES:
CN(C)[C@H]1CN(Cc2c(C)cccc2F)C[C@@H]1c1cn(C)c2ccccc12 |r|
Structure:
