General Information of the Protein
Protein ID
PT02899
Protein Name
Lysine-specific histone demethylase 1A
Secondarily
Protein Name
BRAF35-HDAC complex protein BHC110
Flavin-containing amine oxidase domain-containing protein 2
[histone H3]-dimethyl-L-lysine(4) FAD-dependent demethylase 1A
Gene Name
KDM1A
Secondarily
Gene Name
AOF2
KDM1
KIAA0601
LSD1
Sequence
MLSGKKAAAAAAAAAAAATGTEAGPGTAGGSENGSEVAAQPAGLSGPAEVGPGAVGERTPRKKEPPRASPPGGLAEPPGSAGPQAGPTVVPGSATPMETGIAETPEGRRTSRRKRAKVEYREMDESLANLSEDEYYSEEERNAKAEKEKKLPPPPPQAPPEEENESEPEEPSGVEGAAFQSRLPHDRMTSQEAACFPDIISGPQQTQKVFLFIRNRTLQLWLDNPKIQLTFEATLQQLEAPYNSDTVLVHRVHSYLERHGLINFGIYKRIKPLPTKKTGKVIIIGSGVSGLAAARQLQSFGMDVTLLEARDRVGGRVATFRKGNYVADLGAMVVTGLGGNPMAVVSKQVNMELAKIKQKCPLYEANGQAVPKEKDEMVEQEFNRLLEATSYLSHQLDFNVLNNKPVSLGQALEVVIQLQEKHVKDEQIEHWKKIVKTQEELKELLNKMVNLKEKIKELHQQYKEASEVKPPRDITAEFLVKSKHRDLTALCKEYDELAETQGKLEEKLQELEANPPSDVYLSSRDRQILDWHFANLEFANATPLSTLSLKHWDQDDDFEFTGSHLTVRNGYSCVPVALAEGLDIKLNTAVRQVRYTASGCEVIAVNTRSTSQTFIYKCDAVLCTLPLGVLKQQPPAVQFVPPLPEWKTSAVQRMGFGNLNKVVLCFDRVFWDPSVNLFGHVGSTTASRGELFLFWNLYKAPILLALVAGEAAGIMENISDDVIVGRCLAILKGIFGSSAVPQPKETVVSRWRADPWARGSYSYVAAGSSGNDYDLMAQPITPGPSIPGAPQPIPRLFFAGEHTIRNYPATVHGALLSGLREAGRIADQFLGAMYTLPRQATPGVPAQQSPSM
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Eraser
>
Lysine demethylase
>
Lysine-specific demethylase
Function
Histone demethylase that can demethylate both 'Lys-4' (H3K4me) and 'Lys-9' (H3K9me) of histone H3, thereby acting as a coactivator or a corepressor, depending on the context (PubMed:15620353, PubMed:15811342, PubMed:16140033, PubMed:16079794, PubMed:16079795, PubMed:16223729). Acts by oxidizing the substrate by FAD to generate the corresponding imine that is subsequently hydrolyzed (PubMed:15620353, PubMed:15811342, PubMed:16079794, PubMed:21300290). Acts as a corepressor by mediating demethylation of H3K4me, a specific tag for epigenetic transcriptional activation. Demethylates both mono- (H3K4me1) and di-methylated (H3K4me2) H3K4me (PubMed:15620353, PubMed:20389281, PubMed:21300290, PubMed:23721412). May play a role in the repression of neuronal genes. Alone, it is unable to demethylate H3K4me on nucleosomes and requires the presence of RCOR1/CoREST to achieve such activity (PubMed:16140033, PubMed:16079794, PubMed:16885027, PubMed:21300290, PubMed:23721412). Also acts as a coactivator of androgen receptor (AR)-dependent transcription, by being recruited to AR target genes and mediating demethylation of H3K9me, a specific tag for epigenetic transcriptional repression. The presence of PRKCB in AR-containing complexes, which mediates phosphorylation of 'Thr-6' of histone H3 (H3T6ph), a specific tag that prevents demethylation H3K4me, prevents H3K4me demethylase activity of KDM1A (PubMed:16079795). Demethylates di-methylated 'Lys-370' of p53/TP53 which prevents interaction of p53/TP53 with TP53BP1 and represses p53/TP53-mediated transcriptional activation. Demethylates and stabilizes the DNA methylase DNMT1 (PubMed:29691401). Demethylates methylated 'Lys-42' and methylated 'Lys-117' of SOX2 (PubMed:29358331). Required for gastrulation during embryogenesis. Component of a RCOR/GFI/KDM1A/HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development. Effector of SNAI1-mediated transcription repression of E-cadherin/CDH1, CDN7 and KRT8. Required for the maintenance of the silenced state of the SNAI1 target genes E-cadherin/CDH1 and CDN7 (PubMed:20389281).
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Uniprot ID
Primary ID:
O60341

Secondarily ID:
A8MWP9
Q5TH94
Q5TH95
Q86VT7
Q8IXK4
Q8NDP6
Q8TAZ3
Q96AW4
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Ensembl ID
ENSG00000004487
HGNC ID
HGNC:29079
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: CL000091 , MV4-11
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0520990
 Compound Info 
2-(6-(((1R,2S)-2-((E)-1-phenylbut-1-en-2-yl)cyclopropyl)amino)-2-azaspiro[3.3]heptan-2-yl)ethanol
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C21H30N2O
  1
1
EC50 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0517434
 Compound Info 
2-[4-[[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]amino]piperidin-1-yl]ethanol
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C20H30N2O
  1
1
EC50 = 4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0562204
 Compound Info 
2-(oxetan-3-yl)-N-[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]-2-azaspiro[3.3]heptan-6-amine
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C22H30N2O
  1
1
EC50 = 4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0409944
 Compound Info 
US10517849, Compound 11
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C23H34N2O
  1
1
EC50 = 5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0554223
 Compound Info 
N-[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]-2-azaspiro[3.3]heptan-6-amine
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C19H26N2
  1
1
EC50 = 5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0520991
 Compound Info 
2-[[4-[[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]amino]cyclohexyl]amino]ethanol
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C21H32N2O
  1
1
EC50 = 6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0562215
 Compound Info 
2-methylsulfonyl-N-[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]-2-azaspiro[3.3]heptan-6-amine
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C20H28N2O2S
  1
1
EC50 = 6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0554222
 Compound Info 
2-(2,2-difluoroethyl)-N-[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]-2-azaspiro[3.3]heptan-6-amine
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C21H28F2N2
  1
1
EC50 = 7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0470015
 Compound Info 
1-[6-[[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]amino]-2-azaspiro[3.3]heptan-2-yl]ethanone
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C21H28N2O
  1
1
EC50 = 14 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0421552
 Compound Info 
2-[[4-[[(1R,2S)-2-[(E)-1-phenylprop-1-en-2-yl]cyclopropyl]amino]cyclohexyl]amino]ethanol
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C20H30N2O
  1
1
EC50 = 52 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0121735
 Compound Info 
4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]piperidin-1-yl]methyl]benzoic acid
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C23H28N2O2
  1
1
EC50 = 54 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0517435
 Compound Info 
4-[[(1R,2S)-2-[(E)-1-phenylprop-1-en-2-yl]cyclopropyl]amino]piperidin-2-one
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C17H22N2O
  1
1
EC50 = 173 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0409945
 Compound Info 
N-[(1R,2S)-2-[(E)-1-phenylprop-1-en-2-yl]cyclopropyl]azetidin-3-amine
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C15H20N2
  1
1
EC50 = 312 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0569449
 Compound Info 
4-[[(1R,2S)-2-[(E)-1-phenylprop-1-en-2-yl]cyclopropyl]amino]cyclohexan-1-ol
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C18H25NO
  1
1
EC50 = 327 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0931033
 Compound Info 
(+/-)-N-(1H-imidazol-5-ylmethyl)-2-[(E)-1-methyl-2-phenyl-vinyl]cyclopropanamine
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C16H19N3
  1
1
EC50 = 362 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0562219
 Compound Info 
3-[[4-[[(1R,2S)-2-[(E)-1-phenylbut-1-en-2-yl]cyclopropyl]amino]cyclohexyl]amino]propanoic acid
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C22H32N2O2
  1
1
EC50 = 430 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0554224
 Compound Info 
N-[4-[[(1R,2S)-2-[(E)-1-phenylprop-1-en-2-yl]cyclopropyl]amino]cyclohexyl]acetamide
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C20H28N2O
  1
1
EC50 = 540 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568678
 Compound Info 
CHEMBL4645640
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C21H30N2O2
  1
1
EC50 = 550 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000734 , NCI-H1417
 Cell Line Info 
Cell Line ID: CL000358 , NCI-H69
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000040 , THP-1
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0118041
 Compound Info 
US10214477, Example 5
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C15H22N2
  3
1 IC50 = 0.14 nM
2 IC50 = 33 nM
3 Ki = 50 nM
CP0838514
 Compound Info 
PULRODEMSTAT BESILATE
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C30H29F2N5O5S
  1
1 IC50 = 0.3 nM
CP0553766
 Compound Info 
4-[6-(4-amino-piperidin-1-yl)-4- methyl-5-oxo-3-p-tolyl-4,5- dihydro-pyrazin-2-yl]-2-fluoro- benzonitrile
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C24H24FN5O
  1
1 IC50 = 0.5 nM
CP0238212
 Compound Info 
4-[1-(3-chloro-2-methylindazol-5-yl)-5-methyl-4-[(3S)-3-(methylamino)pyrrolidine-1-carbonyl]imidazol-2-yl]-2-fluorobenzonitrile
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C25H23ClFN7O
  1
1 IC50 = 0.7 nM
CP0568405
 Compound Info 
4-[2-(4-amino-piperidin-1-yl)-5- (4-methoxyphenyl)-1-methyl-6-oxo- 1,6-dihydro-pyrimidin-4-yl]- benzonitrile
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C24H25N5O2
  1
1 IC50 = 0.7 nM
CP0550515
 Compound Info 
4-[2-(4-amino-piperidin-1-yl)-5-(4- methoxyphenyl)-1-methyl-6-oxo- 1,6-dihydropyrimidin-4-yl]- benzonitrile
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C24H24FN5O2
  1
1 IC50 = 0.8 nM
CP0137054
 Compound Info 
4-[1-(3-chloro-2-methylindazol-5-yl)-5-methyl-4-[(3R)-3-(methylamino)piperidine-1-carbonyl]imidazol-2-yl]-2-fluorobenzonitrile
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C26H25ClFN7O
  1
1 IC50 = 1 nM
CP0551796
 Compound Info 
4-[6-(4-aminopiperidin-1-yl)-4- methyl-3-(4-methylphenyl)-5-oxo- 4, 5-dihydropyrazin-2- yl]benzonitrile
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C24H25N5O
  1
1 IC50 = 1.4 nM
CP0557131
 Compound Info 
4-[2-[(3aR,7aS)-1,2,3,3a,4,6,7,7a-octahydropyrrolo[3,2-c]pyridin-5-yl]-5-(4-methylphenyl)pyrimidin-4-yl]benzonitrile
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C25H25N5
  1
1 IC50 = 1.4 nM
CP0568406
 Compound Info 
4-(2-(4-aminopiperidin-1-yl)- 1-methyl-6-oxo-5-p-tolyl-1,6- dihydropyrimidin-4-yl)-benzonitrile
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C24H25N5O
  1
1 IC50 = 1.4 nM
CP0176281
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-1-(3-chloro-2-methylindazol-5-yl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C25H23ClFN7O
  1
1 IC50 = 2 nM
CP0361693
 Compound Info 
4-[5-(4-methylphenyl)-2-[[(3R)-pyrrolidin-3-yl]methyl]pyrimidin-4-yl]benzonitrile
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C23H22N4
  1
1 IC50 = 2 nM
CP0137061
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-5-methyl-1-(1-methylindazol-5-yl)imidazol-2-yl]-2-fluorobenzonitrile
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C25H24FN7O
  1
1 IC50 = 3 nM
CP0268631
 Compound Info 
4-[4-[(3S)-3-aminopyrrolidine-1-carbonyl]-5-methyl-1-(2-methylindazol-5-yl)imidazol-2-yl]-2-fluorobenzonitrile
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C24H22FN7O
  1
1 IC50 = 3 nM
CP0574192
 Compound Info 
4-[2-(4-aminopiperidin-1-yl)-5-(4- methylphenyl)pyrimidin-4- yl]benzonitrile
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C23H23N5
  1
1 IC50 = 3 nM
CP0155012
 Compound Info 
2-fluoro-4-[1-(6-fluoro-2-methylindazol-5-yl)-5-methyl-4-[(3S)-3-(methylamino)pyrrolidine-1-carbonyl]imidazol-2-yl]benzonitrile
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C25H23F2N7O
  1
1 IC50 = 4 nM
CP0349899
 Compound Info 
4-[4-[(3S)-3-aminopyrrolidine-1-carbonyl]-1-(3-fluoro-4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C23H21F2N5O2
  1
1 IC50 = 4 nM
CP0361713
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-1-(4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C24H24FN5O2
  1
1 IC50 = 4 nM
CP0125130
 Compound Info 
2-(4-cyano-3-fluorophenyl)-1-(3-fluoro-4-methoxyphenyl)-5-methyl-N-[(3R)-piperidin-3-yl]imidazole-4-carboxamide
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C24H23F2N5O2
  1
1 IC50 = 5 nM
CP0125134
 Compound Info 
4-[4-[(3S)-3-(dimethylamino)pyrrolidine-1-carbonyl]-5-methyl-1-(2-methylindazol-5-yl)imidazol-2-yl]-2-fluorobenzonitrile
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C26H26FN7O
  1
1 IC50 = 7 nM
CP0158470
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-1-(3-fluoro-4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C24H23F2N5O2
  1
1 IC50 = 7 nM
CP0125129
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-5-methyl-1-(4-methylphenyl)imidazol-2-yl]benzonitrile
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C24H25N5O
  1
1 IC50 = 8 nM
CP0125133
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-5-methyl-1-(2-methylindazol-5-yl)imidazol-2-yl]-2-fluorobenzonitrile
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C25H24FN7O
  1
1 IC50 = 9 nM
CP0031502
 Compound Info 
4-[2-(4-methylphenyl)-5-[[(3R)-pyrrolidin-3-yl]methoxy]pyridin-3-yl]benzonitrile
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C24H23N3O
  3
1 IC50 = 10 nM
2 IC50 = 30 nM
3 Kd = 8 nM
CP0125135
 Compound Info 
2-(4-cyano-3-fluorophenyl)-1-(3-fluoro-4-methoxyphenyl)-5-methyl-N-[(3S)-piperidin-3-yl]imidazole-4-carboxamide
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C24H23F2N5O2
  1
1 IC50 = 10 nM
CP0323785
 Compound Info 
4-[4-[3-(aminomethyl)azetidine-1-carbonyl]-1-(3-fluoro-4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C23H21F2N5O2
  1
1 IC50 = 10 nM
CP0326882
 Compound Info 
4-[4-[(3S)-3-(dimethylamino)pyrrolidine-1-carbonyl]-1-(6-fluoro-2-methylindazol-5-yl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C26H25F2N7O
  1
1 IC50 = 10 nM
CP0219218
 Compound Info 
4-[6-(4-amino-piperidin-1-yl)-4- methyl-5-oxo-3-p-tolyl-4,5- dihydro-pyrazin-2-yl]-3-fluoro- benzonitrile
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C24H24FN5O
  1
1 IC50 = 11 nM
CP0176284
 Compound Info 
4-[4-[(3S)-3-(dimethylamino)pyrrolidine-1-carbonyl]-1-(7-fluoro-2-methylindazol-5-yl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C26H25F2N7O
  1
1 IC50 = 12 nM
CP0125131
 Compound Info 
2-(4-cyano-3-fluorophenyl)-1-(3-fluoro-4-methoxyphenyl)-5-methyl-N-piperidin-4-ylimidazole-4-carboxamide
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C24H23F2N5O2
  1
1 IC50 = 14 nM
CP0238214
 Compound Info 
2-(4-cyano-3-fluorophenyl)-1-(3-fluoro-4-methoxyphenyl)-5-methyl-N-[(3R)-pyrrolidin-3-yl]imidazole-4-carboxamide
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C23H21F2N5O2
  1
1 IC50 = 16 nM
CP0361712
 Compound Info 
4-[4-[(3R)-3-aminopyrrolidine-1-carbonyl]-1-(3-fluoro-4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C23H21F2N5O2
  1
1 IC50 = 17 nM
CP0268628
 Compound Info 
4-[4-[(3S)-3-aminopiperidine-1-carbonyl]-1-(3-fluoro-4-methoxyphenyl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C24H23F2N5O2
  1
1 IC50 = 18 nM
CP0238210
 Compound Info 
2-(4-cyano-3-fluorophenyl)-1-(3-fluoro-4-methoxyphenyl)-5-methyl-N-[(3S)-pyrrolidin-3-yl]imidazole-4-carboxamide
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C23H21F2N5O2
  1
1 IC50 = 24 nM
CP0121735
 Compound Info 
4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]piperidin-1-yl]methyl]benzoic acid
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C23H28N2O2
  4
1 IC50 = 24 nM
2 IC50 = 160 nM
3 IC50 = 1200 nM
4 Ki = 1700 nM
CP0238209
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-1-(6-cyclopropylpyridin-3-yl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C25H25FN6O
  1
1 IC50 = 29 nM
CP0268633
 Compound Info 
4-[4-[(3R)-3-aminopiperidine-1-carbonyl]-1-(6-methoxypyridin-3-yl)-5-methylimidazol-2-yl]-2-fluorobenzonitrile
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C23H23FN6O2
  1
1 IC50 = 38 nM
CP0658215
 Compound Info 
N'-(1-(4-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide
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C19H20ClN3O5S
  1
1 IC50 = 40 nM
CP0658216
 Compound Info 
N-((2-methoxypyridin-3-yl)methyl)-2-phenylcyclopropanamine
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C16H18N2O
  1
1 IC50 = 70 nM
CP0249131
 Compound Info 
(1S,2R)-N-[(2-methoxypyridin-3-yl)methyl]-2-phenylcyclopropan-1-amine
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C16H18N2O
  1
1 IC50 = 98 nM
CP0025575
 Compound Info 
(2S,3S,4S,5R,6S)-6-(5,6-dihydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)-3,4,5-trihydroxy-tetrahydro-2H-pyran-2-carboxylic acid
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C21H18O11
  2
1 IC50 = 3010 nM
2 IC50 = 3550 nM
CP0574478
 Compound Info 
(1S,2R)-2-(4-bromophenyl)cyclopropan-1-amine
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C9H10BrN
  1
1 IC50 = 3700 nM
CP0344567
 Compound Info 
(1S,2R)-(+)-2-phenylcyclopropylamine
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C9H11N
  3
1 IC50 = 6300 nM
2 IC50 = 22000 nM
3 IC50 = 40250 nM
CP0216052
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-6-(aziridin-1-yl)hexanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]acetyl]amino]hexanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]propanoic acid
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C96H174N36O28
  1
1 IC50 = 15600 nM
CP0315174
 Compound Info 
4-[2-(4-methylphenyl)-5-[[(3S)-pyrrolidin-3-yl]methoxy]pyridin-3-yl]benzonitrile
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C24H23N3O
  1
1 Kd = 9 nM
CP0226506
 Compound Info 
4-[[2-(2,7-diazaspiro[3.5]nonan-7-yl)-2-oxoethyl]-[(3-fluoro-4-methoxyphenyl)methyl]amino]benzonitrile
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C24H27FN4O2
  1
1 Kd = 32 nM
CP0226477
 Compound Info 
4-[[2-[4-(aminomethyl)piperidin-1-yl]-2-oxoethyl]-[(3-fluoro-4-methoxyphenyl)methyl]amino]benzonitrile
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C23H27FN4O2
  1
1 Kd = 58 nM
CP0050347
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]amino]-6-hydrazinylhexanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]acetyl]amino]hexanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]propanoic acid
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C94H173N37O28
  2
1 Ki = 4.35 nM
2 Ki = 4400 nM
CP0060235
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-6-[methyl(prop-2-ynyl)amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]acetyl]amino]hexanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]propanoic acid
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C98H176N36O28
  2
1 Ki = 107 nM
2 Ki = 8300 nM
CP0071672
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-6-(prop-2-ynylamino)hexanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]acetyl]amino]hexanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]propanoic acid
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C97H174N36O28
  2
1 Ki = 8300 nM
2 Ki = 16600 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific histone demethylase 1 (LSD) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Lymphoma [ICD-11: 2A80-2A86]
2 Acute myeloid leukaemia [ICD-11: 2A60]
3 Alzheimer disease [ICD-11: 8A20]
4 Small-cell lung cancer [ICD-11: 2C25.Y]
5 Ewing sarcoma [ICD-11: 2B52]
Clinical Trial Drug(s) 6 Clinical Trial Drugs  6
1 CC-90011
 Drug Info 
Phase 2
Lymphoma
2 IMG-7289
 Drug Info 
Phase 2
Acute myeloid leukaemia
3 ORY-2001
 Drug Info 
Phase 2
Alzheimer disease
4 Vafidemstat
 Drug Info 
Phase 2
Alzheimer disease
5 GSK2879552
 Drug Info 
Phase 1
Small-cell lung cancer
6 Seclidemstat
 Drug Info 
Phase 1
Ewing sarcoma