General Information of the Protein
Protein ID
PT03003
Protein Name
Histone-lysine N-methyltransferase EZH2
Secondarily
Protein Name
ENX-1
Enhancer of zeste homolog 2
Lysine N-methyltransferase 6
Gene Name
EZH2
Secondarily
Gene Name
KMT6
Sequence
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
>
Protein methyltransferase
Function
Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' (H3K9me) and 'Lys-27' (H3K27me) of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Displays a preference for substrates with less methylation, loses activity when progressively more methyl groups are incorporated into H3K27, H3K27me0 > H3K27me1 > H3K27me2 (PubMed:22323599, PubMed:30923826). Compared to EZH1-containing complexes, it is more abundant in embryonic stem cells and plays a major role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation. 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, CDKN2A and retinoic acid target genes. EZH2 can also methylate non-histone proteins such as the transcription factor GATA4 and the nuclear receptor RORA. Regulates the circadian clock via histone methylation at the promoter of the circadian genes. Essential for the CRY1/2-mediated repression of the transcriptional activation of PER1/2 by the CLOCK-BMAL1 heterodimer; involved in the di and trimethylation of 'Lys-27' of histone H3 on PER1/2 promoters which is necessary for the CRY1/2 proteins to inhibit transcription.
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Uniprot ID
Primary ID:
Q15910

Secondarily ID:
B2RAQ1
B3KS30
B7Z1D6
B7Z7L6
Q15755
Q75MG3
Q92857
Q96FI6
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Ensembl ID
ENSG00000106462
HGNC ID
HGNC:3527
Subcellular Location
Nucleus
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
CP0004161
 Compound Info 
US10155002, Compound 44
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C34H44N4O4
  1
1
EC50 = 200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0303801
 Compound Info 
5-bromo-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-[methyl(oxan-4-yl)amino]benzamide
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C22H28BrN3O3
  1
1
EC50 = 300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0472310
 Compound Info 
5-chloro-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methylbenzamide
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C23H30ClN3O3
  1
1
EC50 = 300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0303800
 Compound Info 
5-bromo-3-[cyclopentyl(methyl)amino]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylbenzamide
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C22H28BrN3O2
  1
1
EC50 = 500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0269603
 Compound Info 
US10155002, Compound 2
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C33H42N4O3
  1
1
EC50 = 700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0084841
 Compound Info 
1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
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C32H37N5O3
  1
1
EC50 = 2900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0119768
 Compound Info 
EPZ005030
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C29H34N6O3
  1
1
EC50 = 10500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0572229
 Compound Info 
2-[2-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyrimidin-5-yl]-2-cyano-N-(oxetan-3-yl)acetamide
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C27H30ClN7O2
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0577059
 Compound Info 
2-[2-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyrimidin-5-yl]-3-hydroxy-N-(oxetan-3-yl)propanamide
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C27H33ClN6O3
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0578652
 Compound Info 
2-[2-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyrimidin-5-yl]-N-(oxetan-3-yl)acetamide
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C26H31ClN6O2
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0578653
 Compound Info 
2-[6-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyridin-3-yl]-N-(oxetan-3-yl)acetamide
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C27H32ClN5O2
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0579121
 Compound Info 
2-[2-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyrimidin-5-yl]-2,2-difluoro-N-(oxetan-3-yl)acetamide
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C26H29ClF2N6O2
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0579122
 Compound Info 
2-[2-[[4-[(8-chloro-7-methylquinolin-2-yl)amino]cyclohexyl]methylamino]pyrimidin-5-yl]-2-hydroxy-N-(oxetan-3-yl)acetamide
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C26H31ClN6O3
  1
1
IC50 < 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000286 , HCC1806
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000180 , Karpas-422
 Cell Line Info 
Cell Line ID: CL000346 , L-5178-Y
 Cell Line Info 
Cell Line ID: CL000141 , LNCaP
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0119303
 Compound Info 
3-chloro-4-(2-cyano-3-pyridazin-4-ylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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C27H28ClN5O2
  2
1 IC50 = 0.032 nM
2 IC50 = 320 nM
CP0004161
 Compound Info 
US10155002, Compound 44
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C34H44N4O4
  9
1 IC50 = 0.34 nM
2 IC50 = 1 nM
3 IC50 = 4 nM
4 IC50 = 11 nM
5 IC50 = 13.05 nM
6 IC50 = 20 nM
7 IC50 = 150 nM
8 IC50 = 200 nM
9 Ki = 2.5 nM
CP0345528
 Compound Info 
6,9-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-4-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2,3-dihydro-1H-1,4-benzodiazepin-5-one
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C22H22Cl2N4O4
  1
1 IC50 = 0.35 nM
CP0719407
 Compound Info 
(R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(tetrahydro-2H-pyran-4-yl)ethyl)-1H-indole-3-carboxamide
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C25H31N3O4
  3
1 IC50 = 0.5 nM
2 IC50 = 2 nM
3 IC50 = 4 nM
CP0546365
 Compound Info 
6,9-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-4-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-1-methyl-2,3-dihydro-1,4-benzodiazepin-5-one
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C23H24Cl2N4O4
  1
1 IC50 = 0.87 nM
CP0032236
 Compound Info 
1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
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C31H38N6O2
  7
1 IC50 = 1 nM
2 IC50 = 2 nM
3 IC50 = 5.5 nM
4 IC50 = 9.9 nM
5 IC50 = 10 nM
6 IC50 = 12.9 nM
7 Ki = 0.5 nM
CP0663934
 Compound Info 
(R)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(tetrahydro-2H-pyran-4-yl)ethyl)-1H-indole-3-carboxamide
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C25H31N3O3
  2
1 IC50 < 1 nM
2 IC50 = 4 nM
CP0677622
 Compound Info 
(R)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-2-methyl-1H-indole-3-carboxamide
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C27H36N4O4S
  3
1 IC50 = 1 nM
2 IC50 = 2 nM
3 IC50 = 3 nM
CP0751486
 Compound Info 
(R)-1-(1-(1-(2,2-Difluoropropyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
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C28H36F2N4O3
  1
1 IC50 < 1 nM
CP0677621
 Compound Info 
(R)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
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C27H36N4O5S
  4
1 IC50 < 1 nM
2 IC50 = 2 nM
3 IC50 = 2.8 nM
4 IC50 = 3 nM
CP0802162
 Compound Info 
Ethyl (R)-2-(4-(1-(3-(((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-1H-indol-1-yl)ethyl)-piperidin-1-yl)acetate
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C29H38N4O5
  2
1 IC50 < 1 nM
2 IC50 = 2.5 nM
CP0903295
 Compound Info 
Isopropyl (R)-4-(1-(3-(((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-1H-indol-1-yl)ethyl)-piperidine-1-carboxylate
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C29H38N4O5
  2
1 IC50 < 1 nM
2 IC50 = 4.1 nM
CP0903296
 Compound Info 
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-methyl)-2-methyl-1-(1-(1-(oxetan-3-yl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
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C28H36N4O4
  2
1 IC50 < 1 nM
2 IC50 = 1.7 nM
CP0958193
 Compound Info 
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-methyl)-2-methyl-1-(1-(1-methylpiperidin-4-yl)ethyl)-1H-indole-3-carboxamide
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C26H34N4O3
  2
1 IC50 < 1 nM
2 IC50 = 1.7 nM
CP0256275
 Compound Info 
5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1-one
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C22H21Cl2N3O3
  6
1 IC50 = 1 nM
2 IC50 < 5 nM
3 Ki = 0.7 nM
4 Ki = 1 nM
5 Ki = 1.2 nM
6 Ki = 3 nM
CP0025055
 Compound Info 
N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide
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C31H39N7O2
  2
1 IC50 = 1.2 nM
2 Ki = 1.2 nM
CP0833865
 Compound Info 
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-methyl)-2-methyl-1-(1-(1-(2,2,3,3-tetrafluoropropyl)piperidin-4-yl)-ethyl)-1H-indole-3-carboxamide
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C28H34F4N4O3
  2
1 IC50 = 1.6 nM
2 IC50 = 3.3 nM
CP0802164
 Compound Info 
(R)-1-(1-(1-(2,2-Difluoroethyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
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C27H34F2N4O3
  2
1 IC50 = 1.8 nM
2 IC50 = 3.8 nM
CP0659754
 Compound Info 
(R)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-methylpiperidin-4-yl)ethyl)-1H-indole-3-carboxamide
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C26H34N4O2
  2
1 IC50 = 2 nM
2 IC50 = 7 nM
CP0178624
 Compound Info 
N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
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C33H43N7O2
  3
1 IC50 = 2 nM
2 IC50 < 10 nM
3 Ki = 4.6 nM
CP0959692
 Compound Info 
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-methyl)-2-methyl-1-(1-(piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
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C25H32N4O3
  2
1 IC50 = 2 nM
2 IC50 = 3.9 nM
CP0231582
 Compound Info 
Cpi-1205
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C27H33F3N4O3
  4
1 IC50 = 2.2 nM
2 IC50 = 3.1 nM
3 IC50 = 22 nM
4 IC50 = 31 nM
CP0774010
 Compound Info 
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-methyl)-2-methyl-1-(1-(1-(3,3,3-trifluoropropyl)piperidin-4-yl)-ethyl)-1H-indole-3-carboxamide
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C28H35F3N4O3
  2
1 IC50 = 2.3 nM
2 IC50 = 4.8 nM
CP0833864
 Compound Info 
(R)-1-(1-(1-Isobutyrylpiperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
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C29H38N4O4
  2
1 IC50 = 2.5 nM
2 IC50 = 16 nM
CP0751487
 Compound Info 
(R)-1-(1-(1-(Dimethylcarbamoyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
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C28H37N5O4
  2
1 IC50 = 3.3 nM
2 IC50 = 8.9 nM
CP0281730
 Compound Info 
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-[(2R)-1-methoxypropan-2-yl]-2-methylindole-3-carboxamide
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C22H27N3O3
  2
1 IC50 = 5 nM
2 IC50 = 43 nM
CP0659753
 Compound Info 
(R)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-2-methyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indole-3-carboxamide
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C29H40N4O4S
  2
1 IC50 = 5 nM
2 IC50 = 40 nM
CP0677625
 Compound Info 
(R)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-phenylethyl)-1H-indole-3-carboxamide
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C26H27N3O2
  2
1 IC50 = 7 nM
2 IC50 = 34 nM
CP0472310
 Compound Info 
5-chloro-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methylbenzamide
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C23H30ClN3O3
  1
1 IC50 = 10 nM
CP0574241
 Compound Info 
N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide
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C30H38N8O2
  1
1 IC50 = 11 nM
CP0573038
 Compound Info 
(2R)-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-2,4-dimethyl-2-(morpholin-4-ylmethyl)-1,3-benzodioxole-5-carboxamide
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C34H44N6O5
  1
1 IC50 = 11 nM
CP0487679
 Compound Info 
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
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C23H26N4O2
  2
1 IC50 = 13 nM
2 IC50 = 15 nM
CP0124360
 Compound Info 
1-butan-2-yl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylindole-3-carboxamide
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C22H27N3O2
  2
1 IC50 = 14 nM
2 IC50 = 118 nM
CP0572193
 Compound Info 
5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(1,4,6-trimethyl-2-oxopyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1-one
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C23H23Cl2N3O3
  1
1 IC50 = 14 nM
CP0943748
 Compound Info 
7-chloro-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
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C26H34ClN3O4
  1
1 IC50 = 16 nM
CP0968211
 Compound Info 
(R)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
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C27H33F3N4O2
  1
1 IC50 = 22 nM
CP0946240
 Compound Info 
7-bromo-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
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C26H34BrN3O4
  1
1 IC50 = 24 nM
CP0129819
 Compound Info 
3-[cyclopropanecarbonyl(ethyl)amino]-5-[6-[4-(cyclopropylmethyl)piperazin-1-yl]-2-methylpyridin-3-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylbenzamide
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C36H46N6O3
  2
1 IC50 = 26.1 nM
2 IC50 = 72.3 nM
CP0303800
 Compound Info 
5-bromo-3-[cyclopentyl(methyl)amino]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylbenzamide
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C22H28BrN3O2
  1
1 IC50 = 30 nM
CP0303801
 Compound Info 
5-bromo-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-[methyl(oxan-4-yl)amino]benzamide
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C22H28BrN3O3
  1
1 IC50 = 30 nM
CP0497939
 Compound Info 
CHEMBL3394229
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C25H30ClN3O3
  1
1 IC50 = 32 nM
CP0704307
 Compound Info 
(R)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-2-methyl-N-((6-methyl-2-oxo-4-(2,2,2-trifluoroethoxy)-1,2-dihydropyridin-3-yl)methyl)-1H-indole-3-carboxamide
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C28H35F3N4O5S
  2
1 IC50 = 40 nM
2 IC50 = 485 nM
CP0269603
 Compound Info 
US10155002, Compound 2
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C33H42N4O3
  2
1 IC50 = 50 nM
2 IC50 = 54.9 nM
CP0084841
 Compound Info 
1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
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C32H37N5O3
  3
1 IC50 = 54 nM
2 IC50 = 54000 nM
3 Ki = 24 nM
CP0119768
 Compound Info 
EPZ005030
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C29H34N6O3
  2
1 IC50 = 400 nM
2 Ki = 180 nM
CP0011023
 Compound Info 
AdoHcy
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C14H20N6O5S
  3
1 IC50 = 22600 nM
2 IC50 = 23700 nM
3 IC50 = 65000 nM
CP0074148
 Compound Info 
5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one
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C22H24Cl2N2O5
  1
1 Ki < 0.1 nM
CP0567383
 Compound Info 
5-bromo-8-chloro-2-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-7-(3,5-dimethyltriazol-4-yl)-3,4-dihydroisoquinolin-1-one
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C21H21BrClN5O2
  2
1 Ki = 2 nM
2 Ki = 7 nM
CP0028621
 Compound Info 
6-cyclopropyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide
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C21H25N5O2
  1
1 Ki = 700 nM
Clinical Information about the Protein
Target 1 ( Enhancer of zeste homolog 2 (EZH2) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Follicular lymphoma [ICD-11: 2A80]
2 Prostate cancer [ICD-11: 2C82.0]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Small-cell lung cancer [ICD-11: 2C25.Y]
5 Breast cancer [ICD-11: 2C60-2C65]
Approved Drug(s) 1 Approved Drug  1
1 Tazemetostat
 Drug Info 
Approved
Follicular lymphoma
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 CPI-1205
 Drug Info 
Phase 1/2
Prostate cancer
2 GSK2816126
 Drug Info 
Phase 1
Solid tumour/cancer
3 PF-06821497
 Drug Info 
Phase 1
Small-cell lung cancer
Investigative Drug(s) 1 Investigative Drug  1
1 MS1943
 Drug Info 
Investigative
Breast cancer
Target 2 ( EZH2 Y641F mutant (EZH2 Y641F) )
Target Type Patented-recorded Target
Target 3 ( EZH2 Y641N mutant (EZH2 Y641N) )
Target Type Patented-recorded Target