General Information of the Protein
Protein ID
PT03193
Protein Name
Polycomb protein EED
Secondarily
Protein Name
Embryonic ectoderm development protein
WD protein associating with integrin cytoplasmic tails 1
Gene Name
EED
Sequence
MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
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Organism
Homo sapiens, Human
Protein Classification
Unclassified protein
Function
Polycomb group (PcG) protein. Component of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' and 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Also recognizes 'Lys-26' trimethylated histone H1 with the effect of inhibiting PRC2 complex methyltransferase activity on nucleosomal histone H3 'Lys-27', whereas H3 'Lys-27' recognition has the opposite effect, enabling the propagation of this repressive mark. The PRC2/EED-EZH2 complex may also serve as a recruiting platform for DNA methyltransferases, thereby linking two epigenetic repression systems. Genes repressed by the PRC2/EED-EZH2 complex include HOXC8, HOXA9, MYT1 and CDKN2A.
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Uniprot ID
Primary ID:
O75530

Secondarily ID:
A8K7V5
O00149
Q6NTH2
Q7LDA5
Q7LDG8
Q86VV2
Q9UNY7
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Ensembl ID
ENSG00000074266
HGNC ID
HGNC:3188
Subcellular Location
Nucleus
Chromosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000175 , G-401
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0477678
 Compound Info 
[3-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-(3-fluoroazetidin-1-yl)methanone
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C27H32F2N4O
  1
1
IC50 = 31 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0560330
 Compound Info 
N-(furan-2-ylmethyl)-8-[4-(pyrrolidin-1-ylmethyl)phenyl]-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
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C21H22N6O
  1
1
IC50 = 32 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0226502
 Compound Info 
1-[4-[4-[(3S,4R)-4-(dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanone
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C27H35FN4O
  1
1
IC50 = 33 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0004161
 Compound Info 
US10155002, Compound 44
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C34H44N4O4
  1
1
IC50 = 40 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0103693
 Compound Info 
(1S,2R)-4-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-2-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]cyclopentan-1-amine
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C27H36FN3O2S
  1
1
IC50 = 57 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0103694
 Compound Info 
4-[3-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-1-methylpiperazin-2-one
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C28H36FN5O
  1
1
IC50 = 190 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0468096
 Compound Info 
8-(2-fluorophenyl)-5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile
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C18H12FN5O
  1
1
IC50 = 210 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0253551
 Compound Info 
EED226
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C17H15N5O3S
  1
1
IC50 = 220 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0561455
 Compound Info 
6-[4-[(3S,4R)-4-(dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]piperidin-1-yl]pyridine-3-carboxamide
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C26H34FN5O
  1
1
IC50 = 230 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0365496
 Compound Info 
(3R,4S)-1-[(1S)-7-fluoroindan-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine (3)
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C24H28FN3
  1
1
IC50 = 290 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0548466
 Compound Info 
6-(1,3-benzodioxol-4-ylmethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine
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C15H17N3O2
  1
1
IC50 = 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0536118
 Compound Info 
3-(1,3-benzodioxol-4-ylmethyl)piperidine-1-carboximidamide
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C14H19N3O2
  1
1
IC50 = 1600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0455327
 Compound Info 
8-(1,3-benzodioxol-4-ylmethyl)-1-propan-2-yl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine
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C18H23N3O2
  1
1
IC50 = 2000 nM
 Bioactivity Info 
   TI
   LI
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CP0226498
 Compound Info 
rac-(3R,4S)-1-(2-fluoro-6-methylbenzyl)-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine (2)
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C23H28FN3
  1
1
IC50 = 2400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0562607
 Compound Info 
3-(1-benzofuran-7-ylmethyl)piperidine-1-carboximidamide
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C15H19N3O
  1
1
IC50 = 2500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0567290
 Compound Info 
3-(1-benzofuran-4-ylmethyl)piperidine-1-carboximidamide
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C15H19N3O
  1
1
IC50 = 2500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0446927
 Compound Info 
6-[(2-fluoro-5-methoxyphenyl)methyl]-1-propan-2-yl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine
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C18H24FN3O
  1
1
IC50 = 2900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0420352
 Compound Info 
9-benzyl-5-(furan-2-ylmethylamino)-8,10-dihydro-7H-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrile
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C22H20N6O
  1
1
IC50 = 3280 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0226501
 Compound Info 
(3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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C22H25BrFN3
  1
1
IC50 = 4100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0393488
 Compound Info 
(3R,4S)-1-[(2-chloro-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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C22H25ClFN3
  1
1
IC50 = 6900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0538730
 Compound Info 
6-(1-benzofuran-4-ylmethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine
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C16H17N3O
  1
1
IC50 = 12400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000530 , OCI-Ly19
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0567387
 Compound Info 
N-((5-Fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
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C20H17FN6O
  4
1 IC50 = 4.5 nM
2 IC50 = 5 nM
3 IC50 = 60 nM
4 Kd = 0.4 nM
CP0253551
 Compound Info 
EED226
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C17H15N5O3S
  6
1 IC50 = 12.2 nM
2 IC50 = 17.6 nM
3 IC50 = 20 nM
4 IC50 = 23.4 nM
5 IC50 = 45 nM
6 Kd = 82 nM
CP0420352
 Compound Info 
9-benzyl-5-(furan-2-ylmethylamino)-8,10-dihydro-7H-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrile
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C22H20N6O
  1
1 IC50 = 4030 nM
CP0226502
 Compound Info 
1-[4-[4-[(3S,4R)-4-(dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanone
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C27H35FN4O
  3
1 Kd = 4 nM
2 Ki = 0.29 nM
3 Ki = 0.7 nM
CP0226501
 Compound Info 
(3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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C22H25BrFN3
  3
1 Kd = 150 nM
2 Ki = 10 nM
3 Ki = 13 nM
CP0103693
 Compound Info 
(1S,2R)-4-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-2-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]cyclopentan-1-amine
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C27H36FN3O2S
  1
1 Ki = 0.3 nM
CP0561455
 Compound Info 
6-[4-[(3S,4R)-4-(dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]piperidin-1-yl]pyridine-3-carboxamide
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C26H34FN5O
  1
1 Ki = 0.45 nM
CP0103694
 Compound Info 
4-[3-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-1-methylpiperazin-2-one
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C28H36FN5O
  1
1 Ki = 0.74 nM
CP0477678
 Compound Info 
[3-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-(3-fluoroazetidin-1-yl)methanone
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C27H32F2N4O
  1
1 Ki = 1 nM
CP0365496
 Compound Info 
(3R,4S)-1-[(1S)-7-fluoroindan-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine (3)
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C24H28FN3
  2
1 Ki = 1 nM
2 Ki = 11 nM
CP0226498
 Compound Info 
rac-(3R,4S)-1-(2-fluoro-6-methylbenzyl)-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine (2)
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C23H28FN3
  2
1 Ki = 4 nM
2 Ki = 12 nM
CP0393488
 Compound Info 
(3R,4S)-1-[(2-chloro-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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C22H25ClFN3
  1
1 Ki = 53 nM
Clinical Information about the Protein
Target 1 ( Embryonic ectoderm development protein (EED) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Diffuse large B-cell lymphoma [ICD-11: 2A81]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 MAK683
 Drug Info 
Phase 1/2
Diffuse large B-cell lymphoma