General Information of the Protein
Protein ID
PT02613
Protein Name
Lysine-specific demethylase 5A
Secondarily
Protein Name
Histone demethylase JARID1A
Jumonji/ARID domain-containing protein 1A
Retinoblastoma-binding protein 2
[histone H3]-trimethyl-L-lysine(4) demethylase 5A
Gene Name
KDM5A
Secondarily
Gene Name
JARID1A
RBBP2
RBP2
Sequence
MAGVGPGGYAAEFVPPPECPVFEPSWEEFTDPLSFIGRIRPLAEKTGICKIRPPKDWQPPFACEVKSFRFTPRVQRLNELEAMTRVRLDFLDQLAKFWELQGSTLKIPVVERKILDLYALSKIVASKGGFEMVTKEKKWSKVGSRLGYLPGKGTGSLLKSHYERILYPYELFQSGVSLMGVQMPNLDLKEKVEPEVLSTDTQTSPEPGTRMNILPKRTRRVKTQSESGDVSRNTELKKLQIFGAGPKVVGLAMGTKDKEDEVTRRRKVTNRSDAFNMQMRQRKGTLSVNFVDLYVCMFCGRGNNEDKLLLCDGCDDSYHTFCLIPPLPDVPKGDWRCPKCVAEECSKPREAFGFEQAVREYTLQSFGEMADNFKSDYFNMPVHMVPTELVEKEFWRLVSSIEEDVIVEYGADISSKDFGSGFPVKDGRRKILPEEEEYALSGWNLNNMPVLEQSVLAHINVDISGMKVPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPSHAAEQLEEVMRELAPELFESQPDLLHQLVTIMNPNVLMEHGVPVYRTNQCAGEFVVTFPRAYHSGFNQGYNFAEAVNFCTADWLPIGRQCVNHYRRLRRHCVFSHEELIFKMAADPECLDVGLAAMVCKELTLMTEEETRLRESVVQMGVLMSEEEVFELVPDDERQCSACRTTCFLSALTCSCNPERLVCLYHPTDLCPCPMQKKCLRYRYPLEDLPSLLYGVKVRAQSYDTWVSRVTEALSANFNHKKDLIELRVMLEDAEDRKYPENDLFRKLRDAVKEAETCASVAQLLLSKKQKHRQSPDSGRTRTKLTVEELKAFVQQLFSLPCVISQARQVKNLLDDVEEFHERAQEAMMDETPDSSKLQMLIDMGSSLYVELPELPRLKQELQQARWLDEVRLTLSDPQQVTLDVMKKLIDSGVGLAPHHAVEKAMAELQELLTVSERWEEKAKVCLQARPRHSVASLESIVNEAKNIPAFLPNVLSLKEALQKAREWTAKVEAIQSGSNYAYLEQLESLSAKGRPIPVRLEALPQVESQVAAARAWRERTGRTFLKKNSSHTLLQVLSPRTDIGVYGSGKNRRKKVKELIEKEKEKDLDLEPLSDLEEGLEETRDTAMVVAVFKEREQKEIEAMHSLRAANLAKMTMVDRIEEVKFCICRKTASGFMLQCELCKDWFHNSCVPLPKSSSQKKGSSWQAKEVKFLCPLCMRSRRPRLETILSLLVSLQKLPVRLPEGEALQCLTERAMSWQDRARQALATDELSSALAKLSVLSQRMVEQAAREKTEKIISAELQKAAANPDLQGHLPSFQQSAFNRVVSSVSSSPRQTMDYDDEETDSDEDIRETYGYDMKDTASVKSSSSLEPNLFCDEEIPIKSEEVVTHMWTAPSFCAEHAYSSASKSCSQGSSTPRKQPRKSPLVPRSLEPPVLELSPGAKAQLEELMMVGDLLEVSLDETQHIWRILQATHPPSEDRFLHIMEDDSMEEKPLKVKGKDSSEKKRKRKLEKVEQLFGEGKQKSKELKKMDKPRKKKLKLGADKSKELNKLAKKLAKEEERKKKKEKAAAAKVELVKESTEKKREKKVLDIPSKYDWSGAEESDDENAVCAAQNCQRPCKDKVDWVQCDGGCDEWFHQVCVGVSPEMAENEDYICINCAKKQGPVSPGPAPPPSFIMSYKLPMEDLKETS
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Reader
>
Plant homeodomain
Function
Histone demethylase that specifically demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code. 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'. Regulates specific gene transcription through DNA-binding on 5'-CCGCCC-3' motif (PubMed:18270511). May stimulate transcription mediated by nuclear receptors. Involved in transcriptional regulation of Hox proteins during cell differentiation (PubMed:19430464). May participate in transcriptional repression of cytokines such as CXCL12. Plays a role in the regulation of the circadian rhythm and in maintaining the normal periodicity of the circadian clock. In a histone demethylase-independent manner, acts as a coactivator of the CLOCK-BMAL1-mediated transcriptional activation of PER1/2 and other clock-controlled genes and increases histone acetylation at PER1/2 promoters by inhibiting the activity of HDAC1 (By similarity). Seems to act as a transcriptional corepressor for some genes such as MT1F and to favor the proliferation of cancer cells (PubMed:27427228).
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Uniprot ID
Primary ID:
P29375

Secondarily ID:
A8MV76
Q4LE72
Q86XZ1
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HGNC ID
HGNC:9886
Subcellular Location
Nucleus
Nucleolus
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: CL000379 , PC-9
Compound ID Compound Name Compound Formula
CP0396098
US10022354, Example 29
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C15H22N4O2
 1
1
EC50 = 960 nM
   TI
   LI
   LO
   TS
CP0407288
US10022354, Example 152
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C16H24N4O2
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0447049
US10022354, Example 151
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C15H22N4O2
 1
1
EC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0546755
N-[1-(5-propan-2-yl-1H-pyrazole-3-carbonyl)pyrrolidin-3-yl]benzamide
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C18H22N4O2
 1
1
EC50 = 6500 nM
   TI
   LI
   LO
   TS
CP0410701
US10022354, Example 78
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C21H26N6O
 2
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0081050
2-(4-[2-(dimethylamino)ethyl]- 5-[(4- fluorophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C20H21FN4O3
 1
1 IC50 = 3 nM
CP0315103
2-[5-[(4- cyanophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C17H12N4O3
 1
1 IC50 = 4 nM
CP0081048
2-{5-[(4-bromobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12BrN3O3
 1
1 IC50 = 6 nM
CP0164116
CPI-455
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C16H14N4O
 2
1 IC50 = 10 nM
2 IC50 = 20 nM
CP0068191
2-[5-[(4-chloro-2- methoxyphenyl)methoxy]pyrazol- 1-yl]pyridine-4-carboxylic acid
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C17H14ClN3O4
 1
1 IC50 = 12 nM
CP0080566
2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl)isonicotinic acid (N19)
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C17H14ClN3O3
 1
1 IC50 = 13 nM
CP0120868
2-[5-[(4-chlorophenyl)methoxy]pyrazol-1-yl]pyridine-4-carboxylic acid
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C16H12ClN3O3
 1
1 IC50 = 14 nM
CP0134733
CHEMBL3785583
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C17H20N6O
 1
1 IC50 = 15.1 nM
CP0080564
2-{5-[(4-chloro-2- fluorobenzyl)oxy]-1H-pyrazol-1- yl}pyridine-4-carboxylic acid
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C16H11ClFN3O3
 1
1 IC50 = 18 nM
CP0081057
2-[5-[(4-chloro-2- ethoxyphenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C18H16ClN3O4
 1
1 IC50 = 19 nM
CP0080562
2-[4-ethyl-5-[(4- fluorophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C18H16FN3O3
 1
1 IC50 = 29 nM
CP0080567
2-{5-[(4-methylbenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C17H15N3O3
 1
1 IC50 = 32 nM
CP0120871
2-[5-[(4-chloro-2- phenylmethoxyphenyl)methoxy] pyrazol-1-yl]pyridine-4-carboxylic acid
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C23H18ClN3O4
 1
1 IC50 = 32 nM
CP0068188
2-{5-[(4-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
 1
1 IC50 = 38 nM
CP0111516
2-{5-[(4-ethylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridine- 4-carboxylic acid
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C18H17N3O3
 1
1 IC50 = 44 nM
CP0248901
2-[5-[[4-chloro-2- (cyclopropylmethoxy(phenyl] methoxy]pyrazol-1-yl]pyridine- 4-carboxylic acid
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C20H18ClN3O4
 1
1 IC50 = 75 nM
CP0329706
2-[5-[(4-fluorophenyl)methoxy]-4- methylpyrazol-1-yl]pyridine-4- carboxylic acid
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C17H14FN3O3
 1
1 IC50 = 77 nM
CP0239481
2-[5-[(4-fluorophenyl)methoxy]-4-(2-hydroxyethyl)pyrazol-1-yl]pyridine-4-carboxylic acid
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C18H16FN3O4
 1
1 IC50 = 80 nM
CP0068190
2-[5-[1-(4- fluorophenyl)ethoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C17H14FN3O3
 1
1 IC50 = 180 nM
CP0353574
2-(5-{[4- (trifluoromethyl)benzyl]oxy}- 1H-pyrazol-1-yl)pyridine-4- carboxylic acid
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C17H12F3N3O3
 1
1 IC50 = 240 nM
CP0239480
2-{5-[(4-cyclopropylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridine-4- carboxylic acid
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C19H17N3O3
 1
1 IC50 = 250 nM
CP0080560
2-{5-[(2-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
 1
1 IC50 = 270 nM
CP0213961
6-ethyl-7-methoxy-5-methylpyrazolo[1,5-a]pyrimidine-3-carbonitrile
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C11H12N4O
 1
1 IC50 = 324 nM
CP0392139
2-{5-[(3-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
 1
1 IC50 = 430 nM
CP0081054
2-(5-(benzyloxy)-1H-pyrazol-1- yl)isonicotinic acid
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C16H13N3O3
 1
1 IC50 = 550 nM
CP0407403
CHEMBL3786862
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C11H10N4O
 1
1 IC50 = 878 nM
CP0239479
2-{5-[(4-methoxybenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C17H15N3O4
 1
1 IC50 = 1700 nM
CP0045795
3-[hydroxy-[5-[methyl(pentyl)amino]pentanoyl]amino]propanoic acid
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C14H28N2O4
 1
1 IC50 = 2300 nM
CP0035875
2,4 PDCA
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C7H5NO4
 1
1 IC50 = 100000 nM
CP0360983
2-[(2-chlorophenyl)-[2-(1-methylpyrrolidin-2-yl)ethoxy]methyl]-1H-pyrrolo[3,2-b]pyridine-7-carboxylic acid
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C22H24ClN3O3
 1
1 Kd = 150 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 5A (KDM5A) )
Target Type Patented-recorded Target