General Information of the Protein
Protein ID
PT02237
Protein Name
Lysine-specific demethylase 2A
Secondarily
Protein Name
CXXC-type zinc finger protein 8
F-box and leucine-rich repeat protein 11
F-box protein FBL7
F-box protein Lilina
F-box/LRR-repeat protein 11
JmjC domain-containing histone demethylation protein 1A
[Histone-H3]-lysine-36 demethylase 1A
Gene Name
KDM2A
Secondarily
Gene Name
CXXC8
FBL11
FBL7
FBXL11
JHDM1A
KIAA1004
Sequence
MEPEEERIRYSQRLRGTMRRRYEDDGISDDEIEGKRTFDLEEKLHTNKYNANFVTFMEGKDFNVEYIQRGGLRDPLIFKNSDGLGIKMPDPDFTVNDVKMCVGSRRMVDVMDVNTQKGIEMTMAQWTRYYETPEEEREKLYNVISLEFSHTRLENMVQRPSTVDFIDWVDNMWPRHLKESQTESTNAILEMQYPKVQKYCLMSVRGCYTDFHVDFGGTSVWYHIHQGGKVFWLIPPTAHNLELYENWLLSGKQGDIFLGDRVSDCQRIELKQGYTFVIPSGWIHAVYTPTDTLVFGGNFLHSFNIPMQLKIYNIEDRTRVPNKFRYPFYYEMCWYVLERYVYCITNRSHLTKEFQKESLSMDLELNGLESGNGDEEAVDREPRRLSSRRSVLTSPVANGVNLDYDGLGKTCRSLPSLKKTLAGDSSSDCSRGSHNGQVWDPQCAPRKDRQVHLTHFELEGLRCLVDKLESLPLHKKCVPTGIEDEDALIADVKILLEELANSDPKLALTGVPIVQWPKRDKLKFPTRPKVRVPTIPITKPHTMKPAPRLTPVRPAAASPIVSGARRRRVRCRKCKACVQGECGVCHYCRDMKKFGGPGRMKQSCVLRQCLAPRLPHSVTCSLCGEVDQNEETQDFEKKLMECCICNEIVHPGCLQMDGEGLLNEELPNCWECPKCYQEDSSEKAQKRKMEESDEEAVQAKVLRPLRSCDEPLTPPPHSPTSMLQLIHDPVSPRGMVTRSSPGAGPSDHHSASRDERFKRRQLLRLQATERTMVREKENNPSGKKELSEVEKAKIRGSYLTVTLQRPTKELHGTSIVPKLQAITASSANLRHSPRVLVQHCPARTPQRGDEEGLGGEEEEEEEEEEEDDSAEEGGAARLNGRGSWAQDGDESWMQREVWMSVFRYLSRRELCECMRVCKTWYKWCCDKRLWTKIDLSRCKAIVPQALSGIIKRQPVSLDLSWTNISKKQLTWLVNRLPGLKDLLLAGCSWSAVSALSTSSCPLLRTLDLRWAVGIKDPQIRDLLTPPADKPGQDNRSKLRNMTDFRLAGLDITDATLRLIIRHMPLLSRLDLSHCSHLTDQSSNLLTAVGSSTRYSLTELNMAGCNKLTDQTLIYLRRIANVTLIDLRGCKQITRKACEHFISDLSINSLYCLSDEKLIQKIS
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Reader
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Plant homeodomain
Function
Histone demethylase that specifically demethylates 'Lys-36' of histone H3, thereby playing a central role in histone code. Preferentially demethylates dimethylated H3 'Lys-36' residue while it has weak or no activity for mono- and tri-methylated H3 'Lys-36'. May also recognize and bind to some phosphorylated proteins and promote their ubiquitination and degradation. Required to maintain the heterochromatic state. Associates with centromeres and represses transcription of small non-coding RNAs that are encoded by the clusters of satellite repeats at the centromere. Required to sustain centromeric integrity and genomic stability, particularly during mitosis. Regulates circadian gene expression by repressing the transcriptional activator activity of CLOCK-BMAL1 heterodimer and RORA in a catalytically-independent manner (PubMed:26037310).
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Uniprot ID
Primary ID:
Q9Y2K7

Secondarily ID:
D4QA03
E9PIL6
I3VM55
Q49A21
Q4G0M3
Q69YY8
Q9BVH5
Q9H7H5
Q9UK66
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Ensembl ID
ENSG00000173120
HGNC ID
HGNC:13606
Subcellular Location
Nucleus
Nucleoplasm
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0401732
2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C17H12Cl2N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0401733
2-[5-(3-ethoxy-4-fluorophenyl)-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C19H17FN6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0401738
1-[(3,4-dichlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C15H10Cl2N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0401739
1-(3-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C14H9ClN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0411559
2-[1-[2-(2-chlorophenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C18H15ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0411562
1-[(2-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C15H11ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0450662
2-[1-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C18H12ClF3N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0450665
1-[(4-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C15H11ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0450666
1-(2-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C14H9ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0458068
2-[1-[2-(2-ethoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C20H20N6O
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0458222
1-benzyl-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C15H12N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0466685
2-[1-[2-(2-methoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C19H18N6O
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0471451
2-[1-[(2-chlorophenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C17H13ClN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0471536
1-[(3-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C15H11ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0478994
2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C21H19FN6O
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0481779
1-(4-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
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C14H9ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0485473
2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C22H18N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0859546
2-[1-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C21H20N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0948434
2-[1-(1-phenylethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
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C18H16N6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0420753
CHEMBL4542928
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C25H33N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0424289
5-[4-[[hexyl(methyl)amino]methyl]phenyl]-7-oxo-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
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C24H31N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 2A (KDM2A) )
Target Type Literature-reported Target