General Information of the Protein
Protein ID
PT02653
Protein Name
N-lysine methyltransferase SMYD2
Secondarily
Protein Name
HSKM-B
Histone methyltransferase SMYD2
Lysine N-methyltransferase 3C
SET and MYND domain-containing protein 2
Gene Name
SMYD2
Secondarily
Gene Name
KMT3C
Sequence
MRAEGLGGLERFCSPGKGRGLRALQPFQVGDLLFSCPAYAYVLTVNERGNHCEYCFTRKEGLSKCGRCKQAFYCNVECQKEDWPMHKLECSPMVVFGENWNPSETVRLTARILAKQKIHPERTPSEKLLAVKEFESHLDKLDNEKKDLIQSDIAALHHFYSKHLGFPDNDSLVVLFAQVNCNGFTIEDEELSHLGSAIFPDVALMNHSCCPNVIVTYKGTLAEVRAVQEIKPGEEVFTSYIDLLYPTEDRNDRLRDSYFFTCECQECTTKDKDKAKVEIRKLSDPPKAEAIRDMVRYARNVIEEFRRAKHYKSPSELLEICELSQEKMSSVFEDSNVYMLHMMYQAMGVCLYMQDWEGALQYGQKIIKPYSKHYPLYSLNVASMWLKLGRLYMGLEHKAAGEKALKKAIAIMEVAHGKDHPYISEIKQEIESH
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
>
Protein methyltransferase
>
SET domain
Function
Protein-lysine N-methyltransferase that methylates both histones and non-histone proteins, including p53/TP53 and RB1. Specifically trimethylates histone H3 'Lys-4' (H3K4me3) in vivo. The activity requires interaction with HSP90alpha. Shows even higher methyltransferase activity on p53/TP53. Monomethylates 'Lys-370' of p53/TP53, leading to decreased DNA-binding activity and subsequent transcriptional regulation activity of p53/TP53. Monomethylates RB1 at 'Lys-860'.
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Uniprot ID
Primary ID:
Q9NRG4

Secondarily ID:
B2R9P9
I6L9H7
Q4V765
Q5VSH9
Q96AI4
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Ensembl ID
ENSG00000143499
HGNC ID
HGNC:20982
Subcellular Location
Cytoplasm
Cytosol
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: CL000935 , CAL-120
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0096816
 Compound Info 
[3-(4-amino-6-methylimidazo[4,5-c]pyridin-1-yl)-3-methylazetidin-1-yl]-[1-[[1-[(1R)-cyclohept-2-en-1-yl]piperidin-4-yl]methyl]pyrrol-3-yl]methanone
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C29H39N7O
  1
1
IC50 = 1300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 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: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0560912
 Compound Info 
5-[2-[1-[2-(3,4-dichlorophenyl)ethyl]azetidin-3-yl]oxyphenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-3-carboxamide
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C30H34Cl2N4O2
  1
1 IC50 = 12 nM
CP0091740
 Compound Info 
3-cyano-5-[2-[4-[2-(3-methylindol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C36H42N6O
  4
1 IC50 < 15 nM
2 IC50 = 31 nM
3 IC50 = 425 nM
4 IC50 < 1000 nM
CP0344699
 Compound Info 
5-[2-[4-[2-(1H-indol-3-yl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-3-carboxamide
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C33H40N6O
  1
1 IC50 = 17 nM
CP0355893
 Compound Info 
3-cyano-5-[2-[4-[2-(1H-indol-3-yl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C35H40N6O
  2
1 IC50 = 27 nM
2 IC50 = 28 nM
CP0224978
 Compound Info 
3-cyano-5-[2-[4-[2-(3-methylphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C34H41N5O
  1
1 IC50 = 31 nM
CP0344698
 Compound Info 
5-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-3-carboxamide
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C31H37Cl2N5O
  1
1 IC50 = 38 nM
CP0367033
 Compound Info 
5-[2-[4-[(3-methoxyphenyl)methylamino]piperidin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-3-carboxamide
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C32H41N5O2
  1
1 IC50 = 39 nM
CP0528321
 Compound Info 
3-[2-[4-[2-(1H-indol-3-yl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C34H41N5O
  1
1 IC50 = 41 nM
CP0344883
 Compound Info 
3-cyano-5-[2-[4-[2-(3-methoxyphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C34H41N5O2
  1
1 IC50 = 59 nM
CP0266851
 Compound Info 
2-[2-[4-[2-(1H-indol-3-yl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-4-carboxamide
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C33H40N6O
  1
1 IC50 = 62 nM
CP0232183
 Compound Info 
6-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
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C32H37Cl2N7O
  1
1 IC50 = 65 nM
CP0572983
 Compound Info 
3-[2-[4-[2-(4-chlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C32H39ClN4O
  1
1 IC50 = 114 nM
CP0152575
 Compound Info 
N-cyclohexyl-3-[2-(3,4-dichlorophenyl)ethylamino]-N-[2-[2-(5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl)ethylamino]ethyl]propanamide
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C29H38Cl2N4O4
  3
1 IC50 = 120 nM
2 IC50 = 230 nM
3 Kd = 500 nM
CP0496391
 Compound Info 
2-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-4-carboxamide
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C31H37Cl2N5O
  1
1 IC50 = 120 nM
CP0528322
 Compound Info 
3-cyano-5-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C33H37Cl2N5O
  1
1 IC50 = 138 nM
CP0558319
 Compound Info 
3-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C32H38Cl2N4O
  1
1 IC50 = 165 nM
CP0261343
 Compound Info 
3-[2-[4-[2-(3-methylphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C33H42N4O
  1
1 IC50 = 211 nM
CP0491817
 Compound Info 
3-[2-[4-[2-(3-methoxyphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C33H42N4O2
  1
1 IC50 = 273 nM
CP0565951
 Compound Info 
2-[2-[4-[2-(4-chlorophenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-4-carboxamide
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C31H38ClN5O
  1
1 IC50 = 305 nM
CP0274376
 Compound Info 
3-[2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)benzamide
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C32H40N4O
  1
1 IC50 = 339 nM
CP0484190
 Compound Info 
2-[2-[4-[2-(3-methoxyphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-4-carboxamide
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C32H41N5O2
  1
1 IC50 = 440 nM
CP0552549
 Compound Info 
2-[2-[4-[2-(4-methoxyphenyl)ethyl]piperazin-1-yl]phenyl]-N-(3-pyrrolidin-1-ylpropyl)pyridine-4-carboxamide
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C32H41N5O2
  1
1 IC50 = 1050 nM
Clinical Information about the Protein
Target 1 ( SET and MYND domain-containing protein 2 (SMYD2) )
Target Type Preclinical Target
Disease 2 Target-related Diseases  2
1 Lung cancer [ICD-11: 2C25.0]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Preclinical Drug(s) 3 Preclinical Drugs  3
1 A-893
 Drug Info 
Preclinical
Lung cancer
2 AZ505
 Drug Info 
Preclinical
Solid tumour/cancer
3 LLY-507
 Drug Info 
Preclinical
Solid tumour/cancer