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Target
Polycomb protein EED
Ligand
BDBM50573358
Substrate
n/a
Meas. Tech.
ChEMBL_2119454 (CHEMBL4828520)
IC50
1.6±n/a nM
Citation
 Rej, RK; Wang, C; Lu, J; Wang, M; Petrunak, E; Zawacki, KP; McEachern, D; Yang, CY; Wang, L; Li, R; Chinnaswamy, K; Wen, B; Sun, D; Stuckey, JA; Zhou, Y; Chen, J; Tang, G; Wang, S Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression. J Med Chem 64:14540-14556 (2021) [PubMed]  Article 
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:
BDBM50573358
Synonyms:
CHEMBL4849266
Type:
Small organic molecule
Emp. Form.:
C27H26F4N6O3
Mol. Mass.:
558.5274
SMILES:
CC(C)(O)CN1Cc2cc(ncc2C2=CN=C(NCc3c4CCOc4ccc3F)N3C=NC(C23)C1=O)C(F)(F)F |c:33,t:14,16|
Structure:
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