Reaction Details
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Polycomb protein EED
Ligand
BDBM223986
Substrate
n/a
Meas. Tech.
TR-FRET Binding Assay
pH
7.5±0
Temperature
298.15±0 K
Ki
1±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:
BDBM223986
Synonyms:
(3R,4S)-1-[(1S)-7-fluoroindan-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine (3)
Type:
Small organic molecule
Emp. Form.:
C24H28FN3
Mol. Mass.:
377.4976
SMILES:
CN(C)[C@H]1CN(C[C@@H]1c1cn(C)c2ccccc12)[C@H]1CCc2cccc(F)c12 |r|
Structure:
