General Information of the Protein
Protein ID
PT03543
Protein Name
Lysine-specific demethylase 5C
Secondarily
Protein Name
Histone demethylase JARID1C
Jumonji/ARID domain-containing protein 1C
Protein SmcX
Protein Xe169
[histone H3]-trimethyl-L-lysine(4) demethylase 5C
Gene Name
KDM5C
Secondarily
Gene Name
DXS1272E
JARID1C
SMCX
XE169
Sequence
MEPGSDDFLPPPECPVFEPSWAEFRDPLGYIAKIRPIAEKSGICKIRPPADWQPPFAVEVDNFRFTPRIQRLNELEAQTRVKLNYLDQIAKFWEIQGSSLKIPNVERRILDLYSLSKIVVEEGGYEAICKDRRWARVAQRLNYPPGKNIGSLLRSHYERIVYPYEMYQSGANLVQCNTRPFDNEEKDKEYKPHSIPLRQSVQPSKFNSYGRRAKRLQPDPEPTEEDIEKNPELKKLQIYGAGPKMMGLGLMAKDKTLRKKDKEGPECPPTVVVKEELGGDVKVESTSPKTFLESKEELSHSPEPCTKMTMRLRRNHSNAQFIESYVCRMCSRGDEDDKLLLCDGCDDNYHIFCLLPPLPEIPKGVWRCPKCVMAECKRPPEAFGFEQATREYTLQSFGEMADSFKADYFNMPVHMVPTELVEKEFWRLVNSIEEDVTVEYGADIHSKEFGSGFPVSDSKRHLTPEEEEYATSGWNLNVMPVLEQSVLCHINADISGMKVPWLYVGMVFSAFCWHIEDHWSYSINYLHWGEPKTWYGVPSLAAEHLEEVMKKLTPELFDSQPDLLHQLVTLMNPNTLMSHGVPVVRTNQCAGEFVITFPRAYHSGFNQGYNFAEAVNFCTADWLPAGRQCIEHYRRLRRYCVFSHEELICKMAACPEKLDLNLAAAVHKEMFIMVQEERRLRKALLEKGITEAEREAFELLPDDERQCIKCKTTCFLSALACYDCPDGLVCLSHINDLCKCSSSRQYLRYRYTLDELPAMLHKLKVRAESFDTWANKVRVALEVEDGRKRSLEELRALESEARERRFPNSELLQQLKNCLSEAEACVSRALGLVSGQEAGPHRVAGLQMTLTELRAFLDQMNNLPCAMHQIGDVKGVLEQVEAYQAEAREALASLPSSPGLLQSLLERGRQLGVEVPEAQQLQRQVEQARWLDEVKRTLAPSARRGTLAVMRGLLVAGASVAPSPAVDKAQAELQELLTIAERWEEKAHLCLEARQKHPPATLEAIIREAENIPVHLPNIQALKEALAKARAWIADVDEIQNGDHYPCLDDLEGLVAVGRDLPVGLEELRQLELQVLTAHSWREKASKTFLKKNSCYTLLEVLCPCADAGSDSTKRSRWMEKELGLYKSDTELLGLSAQDLRDPGSVIVAFKEGEQKEKEGILQLRRTNSAKPSPLASSSTASSTTSICVCGQVLAGAGALQCDLCQDWFHGRCVSVPRLLSSPRPNPTSSPLLAWWEWDTKFLCPLCMRSRRPRLETILALLVALQRLPVRLPEGEALQCLTERAISWQGRARQALASEDVTALLGRLAELRQRLQAEPRPEEPPNYPAAPASDPLREGSGKDMPKVQGLLENGDSVTSPEKVAPEEGSGKRDLELLSSLLPQLTGPVLELPEATRAPLEELMMEGDLLEVTLDENHSIWQLLQAGQPPDLERIRTLLELEKAERHGSRARGRALERRRRRKVDRGGEGDDPAREELEPKRVRSSGPEAEEVQEEEELEEETGGEGPPAPIPTTGSPSTQENQNGLEPAEGTTSGPSAPFSTLTPRLHLPCPQQPPQQQL
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Plant homeodomain
Function
Histone demethylase that specifically demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code (PubMed:28262558). Does not demethylate histone H3 'Lys-9', H3 'Lys-27', H3 'Lys-36', H3 'Lys-79' or H4 'Lys-20'. Demethylates trimethylated and dimethylated but not monomethylated H3 'Lys-4'. Participates in transcriptional repression of neuronal genes by recruiting histone deacetylases and REST at neuron-restrictive silencer elements. Represses the CLOCK-BMAL1 heterodimer-mediated transcriptional activation of the core clock component PER2 (By similarity).
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Uniprot ID
Primary ID:
P41229

Secondarily ID:
B0QZ44
B4E3I2
F5H3T1
Q5JUX3
Q5JUX4
Q5JUX5
Q7Z5S5
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HGNC ID
HGNC:11114
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: CL000013 , Sf9
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0424289
 Compound Info 
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 = 5.84 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0420753
 Compound Info 
CHEMBL4542928
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C25H33N5O
  1
1
IC50 = 6.24 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0396098
 Compound Info 
US10022354, Example 29
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C15H22N4O2
  1
1
IC50 = 55 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123329
 Compound Info 
GSK467
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C17H13N5O2
  1
1
IC50 = 63.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0722127
 Compound Info 
2-((1-(Cyclohexylmethyl)-1H-pyrazol-4-yl)oxy)pyrido[3,4-d]-pyrimidin-4(3H)-one
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C17H19N5O2
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0088649
 Compound Info 
3-(furan-2-ylmethylamino)pyridine-4-carboxylic acid
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C11H10N2O3
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0675001
 Compound Info 
2-((1-Cyclopentyl-1H-pyrazol-4-yl)oxy)pyrido[3,4-d]-pyrimidin-4(3H)-one
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C15H15N5O2
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0695082
 Compound Info 
2-((6-Isopropylpyridin-3-yl)oxy)pyrido[3,4-d]pyrimidin-4(3H)-one
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C15H14N4O2
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0088651
 Compound Info 
3-[(3-methylthiophen-2-yl)methylamino]pyridine-4-carboxylic acid
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C12H12N2O2S
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0796600
 Compound Info 
2-(4-Chloro-3-hydroxyphenoxy)pyrido[3,4-d]pyrimidin-4(3H)-one
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C13H8ClN3O3
  1
1
IC50 = 199.53 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0553488
 Compound Info 
4-hydrazinyl-4-oxobutanoic acid
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C4H8N2O3
  1
1
IC50 = 480 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0274313
 Compound Info 
4-(2-methylhydrazinyl)-4-oxobutanoic acid
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C5H10N2O3
  1
1
IC50 = 1100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0148151
 Compound Info 
4-(Hydroxyamino)-4-oxobutanoic acid
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C4H7NO4
  1
1
IC50 = 1900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0164116
 Compound Info 
CPI-455
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C16H14N4O
  1
1
IC50 = 3010 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0228023
 Compound Info 
4,6-dioxoheptanoic acid
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C7H10O4
  1
1
IC50 = 4500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0045795
 Compound Info 
3-[hydroxy-[5-[methyl(pentyl)amino]pentanoyl]amino]propanoic acid
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C14H28N2O4
  1
1
IC50 = 28900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0181307
 Compound Info 
2-(1-benzylpyrazol-4-yl)oxy-3H-pyrido[2,3-d]pyrimidin-4-one
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C17H13N5O2
  1
1
IC50 = 31622.78 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0363920
 Compound Info 
4-(dimethylaminooxy)-4-oxobutanoic acid
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C6H11NO4
  1
1
IC50 = 42000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0046395
 Compound Info 
4-oxo-4-(propan-2-ylamino)butanoic acid
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C7H13NO3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0076958
 Compound Info 
4-[(dimethylazaniumyl)amino]-4-oxobutanoate
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C6H12N2O3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0182782
 Compound Info 
(3-carboxypropanoylamino)-trimethylazanium
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C7H15N2O3+
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0274372
 Compound Info 
1-N',1-N',4-N',4-N'-tetramethylbutanedihydrazide
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C8H18N4O2
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0452724
 Compound Info 
4-[dimethylamino(methyl)amino]-4-oxobutanoic acid
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C7H14N2O3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0067096
 Compound Info 
2-[(3-methylthiophen-2-yl)methylamino]pyridine-3-carboxylic acid
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C12H12N2O2S
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0067103
 Compound Info 
2-(furan-2-ylmethylamino)pyridine-3-carboxylic acid
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C11H10N2O3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0164116
 Compound Info 
CPI-455
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C16H14N4O
  1
1 IC50 = 14 nM
CP0088649
 Compound Info 
3-(furan-2-ylmethylamino)pyridine-4-carboxylic acid
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C11H10N2O3
  1
1 IC50 = 79 nM
CP0123329
 Compound Info 
GSK467
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C17H13N5O2
  1
1 IC50 = 4000 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 5C (KDM5C) )
Target Type Literature-reported Target