General Information of the Protein
Protein ID
PT03868
Protein Name
Histone-lysine N-methyltransferase SMYD3
Secondarily
Protein Name
SET and MYND domain-containing protein 3
Zinc finger MYND domain-containing protein 1
Gene Name
SMYD3
Secondarily
Gene Name
ZMYND1
ZNFN3A1
Sequence
MEPLKVEKFATAKRGNGLRAVTPLRPGELLFRSDPLAYTVCKGSRGVVCDRCLLGKEKLMRCSQCRVAKYCSAKCQKKAWPDHKRECKCLKSCKPRYPPDSVRLLGRVVFKLMDGAPSESEKLYSFYDLESNINKLTEDKKEGLRQLVMTFQHFMREEIQDASQLPPAFDLFEAFAKVICNSFTICNAEMQEVGVGLYPSISLLNHSCDPNCSIVFNGPHLLLRAVRDIEVGEELTICYLDMLMTSEERRKQLRDQYCFECDCFRCQTQDKDADMLTGDEQVWKEVQESLKKIEELKAHWKWEQVLAMCQAIISSNSERLPDINIYQLKVLDCAMDACINLGLLEEALFYGTRTMEPYRIFFPGSHPVRGVQVMKVGKLQLHQGMFPQAMKNLRLAFDIMRVTHGREHSLIEDLILLLEECDANIRAS
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
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Protein methyltransferase
>
SET domain
Function
Histone methyltransferase. Specifically methylates 'Lys-4' of histone H3, inducing di- and tri-methylation, but not monomethylation (PubMed:15235609, PubMed:22419068). Also methylates 'Lys-5' of histone H4 (PubMed:22419068). Plays an important role in transcriptional activation as a member of an RNA polymerase complex (PubMed:15235609). Binds DNA containing 5'-CCCTCC-3' or 5'-GAGGGG-3' sequences (PubMed:15235609).
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Uniprot ID
Primary ID:
Q9H7B4

Secondarily ID:
A8K0P0
B1AN38
Q86TL8
Q8N5Z6
Q96AI5
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Ensembl ID
ENSG00000185420
HGNC ID
HGNC:15513
Subcellular Location
Cytoplasm
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: CL000314 , HEK293T/17
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0047806
 Compound Info 
6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluorobutyl)piperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
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C26H34ClF3N4O4S
  1
1
IC50 = 36 nM
 Bioactivity Info 
   TI
   LI
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CP0047805
 Compound Info 
N-((1R,3r,5S)-8-((4-(benzylamino)piperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-6-chloro-2-oxoindoline-5-carboxamide
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C28H34ClN5O4S
  1
1
IC50 = 48 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0566726
 Compound Info 
6-chloro-N-((1R,3r,5S)-8-((4-(dimethylamino)piperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C23H32ClN5O4S
  1
1
IC50 = 300 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0383126
 Compound Info 
N-((1R,3r,5S)-8-((4-aminopiperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-6-methyl-2-oxoindoline-5-carboxamide
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C22H31N5O4S
  1
1
IC50 = 410 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0447963
 Compound Info 
6-chloro-N-((1R,3r,5S)-8-((4-(methylamino)piperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C22H30ClN5O4S
  1
1
IC50 = 420 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0414575
 Compound Info 
N-((1R,3r,5S)-8-(((1-methylpiperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C23H32N4O4S
  1
1
IC50 = 480 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0566725
 Compound Info 
N-((1R,3r,5S)-8-((4-aminopiperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-6-fluoro-2-oxoindoline-5-carboxamide
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C21H28FN5O4S
  1
1
IC50 = 530 nM
 Bioactivity Info 
   TI
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CP0414574
 Compound Info 
6-chloro-2-oxo-N-[(1S,5R)-8-[[(3R)-piperidin-3-yl]methylsulfonyl]-8-azabicyclo[3.2.1]octan-3-yl]-1,3-dihydroindole-5-carboxamide
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C22H29ClN4O4S
  1
1
IC50 = 730 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0452624
 Compound Info 
6-chloro-N-((1R,3r,5S)-8-(((1-(3-hydroxypropyl)piperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C25H35ClN4O5S
  1
1
IC50 = 760 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0566724
 Compound Info 
N-((1R,3r,5S)-8-((4-aminopiperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C21H29N5O4S
  1
1
IC50 = 850 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0472082
 Compound Info 
N-((1R,3r,5S)-8-((4-aminopiperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-6-chloro-2-oxoindoline-5-carboxamide
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C21H28ClN5O4S
  1
1
IC50 = 1100 nM
 Bioactivity Info 
   TI
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CP0475479
 Compound Info 
CHEMBL3798745
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C22H29ClN4O4S
  1
1
IC50 = 1300 nM
 Bioactivity Info 
   TI
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CP0571195
 Compound Info 
N-((1R,3R,5S)-8-(((1r,4R)-4-aminocyclohexyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoindoline-5-carboxamide
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C22H30N4O4S
  1
1
IC50 = 2200 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0475480
 Compound Info 
6-chloro-2-oxo-N-((1R,3r,5S)-8-((piperidin-4-ylmethyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
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C22H29ClN4O4S
  1
1
IC50 = 3200 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0402928
 Compound Info 
2-oxo-N-((1R,3r,5S)-8-((piperidin-4-ylmethyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
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C22H30N4O4S
  1
1
IC50 = 3400 nM
 Bioactivity Info 
   TI
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CP0459466
 Compound Info 
1-methyl-2-oxo-N-((1R,3r,5S)-8-((piperidin-4-ylmethyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
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C23H32N4O4S
  1
1
IC50 = 3900 nM
 Bioactivity Info 
   TI
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CP0561879
 Compound Info 
N-(1-((3-aminopropyl)sulfonyl)piperidin-4-yl)-6-chloro-2-oxoindoline-5-carboxamide
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C17H23ClN4O4S
  1
1
IC50 = 6800 nM
 Bioactivity Info 
   TI
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CP0383127
 Compound Info 
N-(1-((3-aminopropyl)sulfonyl)piperidin-4-yl)-2-oxoindoline-5-carboxamide
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C17H24N4O4S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0475481
 Compound Info 
2-oxo-N-(1-((piperidin-4-ylmethyl)sulfonyl)piperidin-4-yl)indoline-5-carboxamide
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C20H28N4O4S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0561880
 Compound Info 
2-oxo-N-(piperidin-4-yl)indoline-5-carboxamide
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C14H17N3O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000063 , Hep-G2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0076206
 Compound Info 
propyl (2R)-4-[2-[4-(1-aminocyclopropyl)phenyl]-4-chloroquinoline-7-carbonyl]-2-methylpiperazine-1-carboxylate
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C28H31ClN4O3
  2
1 IC50 = 11.7 nM
2 Ki = 440 nM
CP0224428
 Compound Info 
CHEMBL4460946
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C23H35F3N4O4S
  2
1 IC50 = 67 nM
2 Ki = 6 nM
CP0352195
 Compound Info 
5-cyclopropyl-N-(1-piperidin-4-ylsulfonylpiperidin-4-yl)-1,2-oxazole-3-carboxamide
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C17H26N4O4S
  2
1 IC50 = 167 nM
2 Ki = 17 nM
CP0462113
 Compound Info 
propyl (2R)-4-(4-chloro-2-phenylquinoline-7-carbonyl)-2-methylpiperazine-1-carboxylate
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C25H26ClN3O3
  1
1 IC50 = 170 nM
CP0076205
 Compound Info 
propyl 4-[4-chloro-2-[4-(methylcarbamoyl)phenyl]quinoline-7-carbonyl]piperazine-1-carboxylate
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C26H27ClN4O4
  2
1 IC50 = 250 nM
2 Ki = 3060 nM
CP0484214
 Compound Info 
propyl 4-[4-chloro-2-(4-methoxyphenyl)quinoline-7-carbonyl]piperazine-1-carboxylate
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C25H26ClN3O4
  1
1 IC50 = 260 nM
CP0252210
 Compound Info 
propyl 4-(4-chloro-2-phenylquinoline-7-carbonyl)piperazine-1-carboxylate
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C24H24ClN3O3
  2
1 IC50 = 300 nM
2 Ki = 3900 nM
CP0143601
 Compound Info 
ethyl 4-(9-chloro-5,6,7,8-tetrahydroacridine-3-carbonyl)piperazine-1-carboxylate
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C21H24ClN3O3
  1
1 IC50 = 4780 nM
CP0145225
 Compound Info 
CHEMBL4476167
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C22H33F3N4O4S
  1
1 Ki = 18 nM
Clinical Information about the Protein
Target 1 ( Histone-lysine N-methyltransferase SMYD3 (SMYD3) )
Target Type Preclinical Target