General Information of the Protein
Protein ID
PT01566
Protein Name
Histone-lysine N-methyltransferase EHMT2
Secondarily
Protein Name
Euchromatic histone-lysine N-methyltransferase 2
HLA-B-associated transcript 8
Histone H3-K9 methyltransferase 3
Lysine N-methyltransferase 1C
Protein G9a
Gene Name
EHMT2
Secondarily
Gene Name
BAT8
C6orf30
G9A
KMT1C
NG36
Sequence
MAAAAGAAAAAAAEGEAPAEMGALLLEKETRGATERVHGSLGDTPRSEETLPKATPDSLEPAGPSSPASVTVTVGDEGADTPVGATPLIGDESENLEGDGDLRGGRILLGHATKSFPSSPSKGGSCPSRAKMSMTGAGKSPPSVQSLAMRLLSMPGAQGAAAAGSEPPPATTSPEGQPKVHRARKTMSKPGNGQPPVPEKRPPEIQHFRMSDDVHSLGKVTSDLAKRRKLNSGGGLSEELGSARRSGEVTLTKGDPGSLEEWETVVGDDFSLYYDSYSVDERVDSDSKSEVEALTEQLSEEEEEEEEEEEEEEEEEEEEEEEEDEESGNQSDRSGSSGRRKAKKKWRKDSPWVKPSRKRRKREPPRAKEPRGVNGVGSSGPSEYMEVPLGSLELPSEGTLSPNHAGVSNDTSSLETERGFEELPLCSCRMEAPKIDRISERAGHKCMATESVDGELSGCNAAILKRETMRPSSRVALMVLCETHRARMVKHHCCPGCGYFCTAGTFLECHPDFRVAHRFHKACVSQLNGMVFCPHCGEDASEAQEVTIPRGDGVTPPAGTAAPAPPPLSQDVPGRADTSQPSARMRGHGEPRRPPCDPLADTIDSSGPSLTLPNGGCLSAVGLPLGPGREALEKALVIQESERRKKLRFHPRQLYLSVKQGELQKVILMLLDNLDPNFQSDQQSKRTPLHAAAQKGSVEICHVLLQAGANINAVDKQQRTPLMEAVVNNHLEVARYMVQRGGCVYSKEEDGSTCLHHAAKIGNLEMVSLLLSTGQVDVNAQDSGGWTPIIWAAEHKHIEVIRMLLTRGADVTLTDNEENICLHWASFTGSAAIAEVLLNARCDLHAVNYHGDTPLHIAARESYHDCVLLFLSRGANPELRNKEGDTAWDLTPERSDVWFALQLNRKLRLGVGNRAIRTEKIICRDVARGYENVPIPCVNGVDGEPCPEDYKYISENCETSTMNIDRNITHLQHCTCVDDCSSSNCLCGQLSIRCWYDKDGRLLQEFNKIEPPLIFECNQACSCWRNCKNRVVQSGIKVRLQLYRTAKMGWGVRALQTIPQGTFICEYVGELISDAEADVREDDSYLFDLDNKDGEVYCIDARYYGNISRFINHLCDPNIIPVRVFMLHQDLRFPRIAFFSSRDIRTGEELGFDYGDRFWDIKSKYFTCQCGSEKCKHSAEAIALEQSRLARLDPHPELLPELGSLPPVNT
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
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Protein methyltransferase
Function
Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones. Also mediates monomethylation of 'Lys-56' of histone H3 (H3K56me1) in G1 phase, leading to promote interaction between histone H3 and PCNA and regulating DNA replication. Also weakly methylates 'Lys-27' of histone H3 (H3K27me). Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently. Probably targeted to histone H3 by different DNA-binding proteins like E2F6, MGA, MAX and/or DP1. May also methylate histone H1. In addition to the histone methyltransferase activity, also methylates non-histone proteins: mediates dimethylation of 'Lys-373' of p53/TP53. Also methylates CDYL, WIZ, ACIN1, DNMT1, HDAC1, ERCC6, KLF12 and itself. Recruited to the promoters of target genes through interaction with transcriptional repressor MSX1, leading to the inhibition of myoblast differentiation via transcriptional repression of differentiation factors (By similarity).
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Uniprot ID
Primary ID:
Q96KQ7

Secondarily ID:
B0UZY2
Q14349
Q5JP83
Q5JQ92
Q5JQA1
Q5JQG3
Q6PK06
Q96MH5
Q96QD0
Q9UQL8
Q9Y331
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Ensembl ID
ENSG00000204371
HGNC ID
HGNC:14129
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: CL000237 , 22Rv1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0042224
 Compound Info 
N-(1-cyclohexylpiperidin-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
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C36H59N7O2
  1
1
IC50 = 14 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0341308
 Compound Info 
N-[1-(cyclohexylmethyl)piperidin-4-yl]-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
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C37H61N7O2
  1
1
IC50 = 24 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0046275
 Compound Info 
2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H47N5O2
  1
1
IC50 = 48 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000067 , HCT 116
 Cell Line Info 
Cell Line ID: CL000411 , IMR-90
 Cell Line Info 
Cell Line ID: CL000083 , MCF-7
 Cell Line Info 
Cell Line ID: CL000111 , MDA-MB-231
 Cell Line Info 
Cell Line ID: CL000206 , PANC-1
 Cell Line Info 
Cell Line ID: CL000048 , PC-3
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0291908
 Compound Info 
6-methoxy-2-(4-propan-2-yl-1,4-diazepan-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C32H53N7O2
  1
1 IC50 = 2 nM
CP0046275
 Compound Info 
2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H47N5O2
  11
1 IC50 < 2.5 nM
2 IC50 = 2.5 nM
3 IC50 = 12 nM
4 IC50 < 15 nM
5 IC50 = 15 nM
6 IC50 = 25 nM
7 IC50 = 30 nM
8 IC50 = 55 nM
9 IC50 = 610 nM
10 Ki = 3.7 nM
11 Ki = 18 nM
CP0154811
 Compound Info 
2-(4,4-difluoropiperidin-1-yl)-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C29H44F2N6O2
  4
1 IC50 < 2.5 nM
2 IC50 = 220 nM
3 Kd = 230 nM
4 Ki = 3.7 nM
CP0158696
 Compound Info 
2-(azepan-1-yl)-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H48N6O2
  2
1 IC50 < 2.5 nM
2 IC50 = 20 nM
CP0203470
 Compound Info 
6-methoxy-2-piperidin-1-yl-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C29H46N6O2
  2
1 IC50 < 2.5 nM
2 IC50 = 16 nM
CP0338455
 Compound Info 
6-methoxy-2-morpholin-4-yl-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C28H44N6O3
  1
1 IC50 < 2.5 nM
CP0016974
 Compound Info 
5'-methoxy-6'-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3'-indole]-2'-amine
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C19H27N3O2
  3
1 IC50 = 2.8 nM
2 IC50 = 3 nM
3 IC50 = 3.3 nM
CP0209417
 Compound Info 
N-(1-cyclopropylpiperidin-4-yl)-2-(4,4-difluoropiperidin-1-yl)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C29H42F2N6O2
  1
1 IC50 = 3 nM
CP0341308
 Compound Info 
N-[1-(cyclohexylmethyl)piperidin-4-yl]-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
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C37H61N7O2
  1
1 IC50 = 4 nM
CP0242458
 Compound Info 
N-(1-cyclopropylpiperidin-4-yl)-2-(1,1-dioxo-1,4-thiazinan-4-yl)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C28H42N6O4S
  1
1 IC50 = 4 nM
CP0281324
 Compound Info 
2-(4-ethyl-1,4-diazepan-1-yl)-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C31H51N7O2
  1
1 IC50 = 5 nM
CP0042224
 Compound Info 
N-(1-cyclohexylpiperidin-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
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C36H59N7O2
  1
1 IC50 = 6 nM
CP0350263
 Compound Info 
2-[4-(cyclohexylmethyl)-1,4-diazepan-1-yl]-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C36H59N7O2
  1
1 IC50 = 7 nM
CP0222876
 Compound Info 
6-Methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
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C28H45N7O2
  2
1 IC50 = 8 nM
2 IC50 = 11000 nM
CP0281327
 Compound Info 
6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C33H55N7O2
  1
1 IC50 = 8 nM
CP0231500
 Compound Info 
7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C27H45N7O3
  2
1 IC50 = 9 nM
2 IC50 = 6000 nM
CP0350264
 Compound Info 
2-(4-benzyl-1,4-diazepan-1-yl)-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C36H53N7O2
  1
1 IC50 = 9 nM
CP0224989
 Compound Info 
6-methoxy-2-(oxan-4-yl)-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C29H45N5O3
  1
1 IC50 = 9 nM
CP0281325
 Compound Info 
6-methoxy-2-(4-phenyl-1,4-diazepan-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C35H51N7O2
  1
1 IC50 = 10 nM
CP0290010
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H49N7O2
  1
1 IC50 = 10 nM
CP0241960
 Compound Info 
N-(1-cyclohexylpiperidin-4-yl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
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C34H55N7O2
  1
1 IC50 = 11 nM
CP0039320
 Compound Info 
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C26H43N7O2
  6
1 IC50 = 15 nM
2 IC50 = 43 nM
3 IC50 = 57 nM
4 IC50 = 43000 nM
5 Kd = 23 nM
6 Ki = 2.6 nM
CP0040710
 Compound Info 
6-Methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
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C29H47N7O2
  2
1 IC50 = 20 nM
2 IC50 = 25 nM
CP0345772
 Compound Info 
2-cyclohexyl-7-[2-[2-(dimethylamino)ethoxy]ethoxy]-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C29H47N5O3
  1
1 IC50 = 21 nM
CP0241952
 Compound Info 
2-(4-cyclohexyl-1,4-diazepan-1-yl)-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C35H57N7O2
  1
1 IC50 = 22 nM
CP0344006
 Compound Info 
2-(azepan-1-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C31H50N6O2
  1
1 IC50 = 31 nM
CP0040703
 Compound Info 
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
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C28H38N6O2
  10
1 IC50 = 67 nM
2 IC50 = 110 nM
3 IC50 = 180 nM
4 IC50 = 290 nM
5 IC50 = 1200 nM
6 IC50 = 1700 nM
7 IC50 = 1900 nM
8 IC50 = 2000 nM
9 IC50 = 2700 nM
10 Kd = 130 nM
CP0043967
 Compound Info 
2-cyclohexyl-6-methoxy-7-(3-piperidin-1-ylpropoxy)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C31H49N5O2
  1
1 IC50 = 110 nM
Clinical Information about the Protein
Target 1 ( Histone-lysine N-methyltransferase EHMT2 (EHMT2) )
Target Type Preclinical Target
Disease 3 Target-related Diseases  3
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Breast cancer [ICD-11: 2C60-2C65]
3 Inflammation [ICD-11: 1A00-CA43.1]
Preclinical Drug(s) 3 Preclinical Drugs  3
1 A-366
 Drug Info 
Preclinical
Solid tumour/cancer
2 BIX-01294
 Drug Info 
Preclinical
Breast cancer
3 MS012
 Drug Info 
Preclinical
Inflammation