General Information of the Protein
Protein ID
PT01123
Protein Name
Lysine-specific demethylase 4A
Secondarily
Protein Name
JmjC domain-containing histone demethylation protein 3A
Jumonji domain-containing protein 2A
[histone H3]-trimethyl-L-lysine(36) demethylase 4A
[histone H3]-trimethyl-L-lysine(9) demethylase 4A
Gene Name
KDM4A
Secondarily
Gene Name
JHDM3A
JMJD2
JMJD2A
KIAA0677
Sequence
MASESETLNPSARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYDDIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPRYSEFEELERKYWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLVEKESGITIEGVNTPYLYFGMWKTSFAWHTEDMDLYSINYLHFGEPKSWYSVPPEHGKRLERLAKGFFPGSAQSCEAFLRHKMTLISPLMLKKYGIPFDKVTQEAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYGKQAVLCSCRKDMVKISMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFLKESELPPRAGNEEECPEEDMEGVEDGEEGDLKTSLAKHRIGTKRHRVCLEIPQEVSQSELFPKEDLSSEQYEMTECPAALAPVRPTHSSVRQVEDGLTFPDYSDSTEVKFEELKNVKLEEEDEEEEQAAAALDLSVNPASVGGRLVFSGSKKKSSSSLGSGSSRDSISSDSETSEPLSCRAQGQTGVLTVHSYAKGDGRVTVGEPCTRKKGSAARSFSERELAEVADEYMFSLEENKKSKGRRQPLSKLPRHHPLVLQECVSDDETSEQLTPEEEAEETEAWAKPLSQLWQNRPPNFEAEKEFNETMAQQAPHCAVCMIFQTYHQVEFGGFNQNCGNASDLAPQKQRTKPLIPEMCFTSTGCSTDINLSTPYLEEDGTSILVSCKKCSVRVHASCYGVPPAKASEDWMCSRCSANALEEDCCLCSLRGGALQRANDDRWVHVSCAVAILEARFVNIAERSPVDVSKIPLPRFKLKCIFCKKRRKRTAGCCVQCSHGRCPTAFHVSCAQAAGVMMQPDDWPFVVFITCFRHKIPNLERAKGALQSITAGQKVISKHKNGRFYQCEVVRLTTETFYEVNFDDGSFSDNLYPEDIVSQDCLQFGPPAEGEVVQVRWTDGQVYGAKFVASHPIQMYQVEFEDGSQLVVKRDDVYTLDEELPKRVKSRLSVASDMRFNEIFTEKEVKQEKKRQRVINSRYREDYIEPALYRAIME
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Methyl-lysine/arginine binding protein
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Tudor domain
Function
Histone demethylase that specifically demethylates 'Lys-9' and 'Lys-36' residues of histone H3, thereby playing a central role in histone code (PubMed:26741168). Does not demethylate histone H3 'Lys-4', H3 'Lys-27' nor H4 'Lys-20'. Demethylates trimethylated H3 'Lys-9' and H3 'Lys-36' residue, while it has no activity on mono- and dimethylated residues. Demethylation of Lys residue generates formaldehyde and succinate. Participates in transcriptional repression of ASCL2 and E2F-responsive promoters via the recruitment of histone deacetylases and NCOR1, respectively.
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Uniprot ID
Primary ID:
O75164

Secondarily ID:
Q5VVB1
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Ensembl ID
ENSG00000066135
HGNC ID
HGNC:22978
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: CL000017 , HeLa
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0138240
 Compound Info 
8-[4-(2-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylethyl)pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C25H26N6O
  1
1
EC50 = 4700 nM
 Bioactivity Info 
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CP0236794
 Compound Info 
8-[4-[2-[4-(3-chlorophenyl)-4-methylpiperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C24H25ClN6O
  1
1
EC50 = 5900 nM
 Bioactivity Info 
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CP0061173
 Compound Info 
8-[4-[2-[4-(3-chlorophenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C23H23ClN6O
  1
1
EC50 = 8500 nM
 Bioactivity Info 
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CP0236796
 Compound Info 
8-[4-[2-[4-(3-pyridin-3-ylphenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C28H27N7O
  1
1
EC50 = 10400 nM
 Bioactivity Info 
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CP0138214
 Compound Info 
8-[4-[2-[4-[3-[2-(dimethylamino)ethyl]phenyl]piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C27H33N7O
  1
1
EC50 = 30300 nM
 Bioactivity Info 
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CP0124532
 Compound Info 
(3R,6S,9S,12S,15S,18S,24S,27S,30S,33S,36S,39S,42R)-12,33-dibenzyl-18-[(2S)-butan-2-yl]-27,30,36-tris(3-carbamimidamidopropyl)-39-[(1S)-1-hydroxyethyl]-24-(hydroxymethyl)-6,9,42-tris[(4-hydroxyphenyl)methyl]-5,8,11,14,17,20,23,26,29,32,35,38,41,44-tetradecaoxo-15-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37,40,43-tetradecazacyclopentatetracontane-3-carboxamide
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C88H124N24O20S
  1
1
EC50 > 50000 nM
 Bioactivity Info 
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CP0124874
 Compound Info 
(3S,9R,12S,15S,18S,21R,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-10,21-dimethyl-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C73H116N26O15S
  1
1
EC50 > 50000 nM
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CP0144864
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C77H114N24O15S
  1
1
EC50 > 50000 nM
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CP0248488
 Compound Info 
(3S,9R,12S,15S,18S,21R,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-21-methyl-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C72H114N26O15S
  1
1
EC50 > 50000 nM
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CP0369631
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-4-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1
EC50 > 50000 nM
 Bioactivity Info 
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CP0369687
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-34-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1
EC50 > 50000 nM
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CP0543535
 Compound Info 
(3R,6S,9S,12S,15R,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-4,15,34-trimethyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C80H120N24O15S
  1
1
EC50 > 50000 nM
 Bioactivity Info 
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CP0545918
 Compound Info 
(3S,9R,12S,15S,18S,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-10-methyl-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C72H114N26O15S
  1
1
EC50 > 50000 nM
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CP0569183
 Compound Info 
(3S,9R,12S,15S,18S,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C71H112N26O15S
  1
1
EC50 > 50000 nM
 Bioactivity Info 
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CP0574848
 Compound Info 
(3R,6S,9S,12S,15R,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-15-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1
EC50 > 50000 nM
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Cell Line ID: CL000043 , U2OS
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0138214
 Compound Info 
8-[4-[2-[4-[3-[2-(dimethylamino)ethyl]phenyl]piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C27H33N7O
  12
1 IC50 = 13 nM
2 IC50 = 17 nM
3 IC50 = 25 nM
4 IC50 = 39 nM
5 IC50 = 60 nM
6 IC50 = 108 nM
7 IC50 = 204 nM
8 IC50 = 346 nM
9 IC50 = 758 nM
10 IC50 = 1842 nM
11 IC50 = 4286 nM
12 Ki = 2 nM
CP0138240
 Compound Info 
8-[4-(2-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylethyl)pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C25H26N6O
  12
1 IC50 = 15 nM
2 IC50 = 22 nM
3 IC50 = 25 nM
4 IC50 = 39 nM
5 IC50 = 61 nM
6 IC50 = 114 nM
7 IC50 = 197 nM
8 IC50 = 423 nM
9 IC50 = 657 nM
10 IC50 = 857 nM
11 IC50 = 2211 nM
12 Ki = 4 nM
CP0058246
 Compound Info 
8-hydroxyquinoline-5-carboxylic acid
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C10H7NO3
  2
1 IC50 = 1700 nM
2 IC50 = 3200 nM
CP0005167
 Compound Info 
CHEBI:49005
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C21H15N3O4
  3
1 IC50 = 3220 nM
2 IC50 = 3330 nM
3 IC50 = 4760 nM
CP0124532
 Compound Info 
(3R,6S,9S,12S,15S,18S,24S,27S,30S,33S,36S,39S,42R)-12,33-dibenzyl-18-[(2S)-butan-2-yl]-27,30,36-tris(3-carbamimidamidopropyl)-39-[(1S)-1-hydroxyethyl]-24-(hydroxymethyl)-6,9,42-tris[(4-hydroxyphenyl)methyl]-5,8,11,14,17,20,23,26,29,32,35,38,41,44-tetradecaoxo-15-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37,40,43-tetradecazacyclopentatetracontane-3-carboxamide
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C88H124N24O20S
  1
1 Kd = 2.6 nM
CP0574848
 Compound Info 
(3R,6S,9S,12S,15R,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-15-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1 Kd = 3.1 nM
CP0369631
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-4-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1 Kd = 8.3 nM
CP0545918
 Compound Info 
(3S,9R,12S,15S,18S,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-10-methyl-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C72H114N26O15S
  1
1 Kd = 9 nM
CP0248488
 Compound Info 
(3S,9R,12S,15S,18S,21R,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-21-methyl-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C72H114N26O15S
  1
1 Kd = 14 nM
CP0369687
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-34-methyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C78H116N24O15S
  1
1 Kd = 14 nM
CP0543535
 Compound Info 
(3R,6S,9S,12S,15R,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-4,15,34-trimethyl-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C80H120N24O15S
  1
1 Kd = 23 nM
CP0144864
 Compound Info 
(3R,6S,9S,12S,18S,21S,24S,27S,30S,33S,36S)-27,33-bis[(2S)-butan-2-yl]-21,24,30-tris(3-carbamimidamidopropyl)-18-(hydroxymethyl)-36-[(4-hydroxyphenyl)methyl]-6,12-bis(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide
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C77H114N24O15S
  1
1 Kd = 42 nM
CP0569183
 Compound Info 
(3S,9R,12S,15S,18S,24S,27S,30S,33S,36S,39S)-18,33-bis[(2S)-butan-2-yl]-15,27,30,36-tetrakis(3-carbamimidamidopropyl)-24-(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,11,14,17,20,23,26,29,32,35,38-dodecaoxo-7-thia-1,4,10,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-9-carboxamide
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C71H112N26O15S
  1
1 Kd > 300 nM
CP0061173
 Compound Info 
8-[4-[2-[4-(3-chlorophenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C23H23ClN6O
  1
1 Ki = 3 nM
CP0236796
 Compound Info 
8-[4-[2-[4-(3-pyridin-3-ylphenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C28H27N7O
  1
1 Ki = 3 nM
CP0236794
 Compound Info 
8-[4-[2-[4-(3-chlorophenyl)-4-methylpiperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C24H25ClN6O
  1
1 Ki = 5 nM
CP0391105
 Compound Info 
4-[(E)-2-[1-[(4-fluorophenyl)methyl]pyridin-1-ium-4-yl]ethenyl]-N,N-dimethylaniline;iodide
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C22H22FIN2
  1
1 Ki = 420 nM
CP0414504
 Compound Info 
2-benzoyl-4-(4-methylphenyl)-9-phenyl-1,6-dithia-3,4,9-triazaspiro[4.4]non-2-en-8-one
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C24H19N3O2S2
  1
1 Ki = 420 nM
CP0477996
 Compound Info 
4-[2-(1-hexylpyridin-1-ium-2-yl)ethenyl]-N,N-dimethylaniline;iodide
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C21H29IN2
  1
1 Ki = 420 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 4A (KDM4A) )
Target Type Patented-recorded Target