General Information of the Protein
Protein ID
PT02221
Protein Name
Histone-lysine N-methyltransferase EHMT1
Secondarily
Protein Name
Euchromatic histone-lysine N-methyltransferase 1
G9a-like protein 1
Histone H3-K9 methyltransferase 5
Lysine N-methyltransferase 1D
Gene Name
EHMT1
Secondarily
Gene Name
EUHMTASE1
GLP
KIAA1876
KMT1D
Sequence
MAAADAEAVPARGEPQQDCCVKTELLGEETPMAADEGSAEKQAGEAHMAADGETNGSCENSDASSHANAAKHTQDSARVNPQDGTNTLTRIAENGVSERDSEAAKQNHVTADDFVQTSVIGSNGYILNKPALQAQPLRTTSTLASSLPGHAAKTLPGGAGKGRTPSAFPQTPAAPPATLGEGSADTEDRKLPAPGADVKVHRARKTMPKSVVGLHAASKDPREVREARDHKEPKEEINKNISDFGRQQLLPPFPSLHQSLPQNQCYMATTKSQTACLPFVLAAAVSRKKKRRMGTYSLVPKKKTKVLKQRTVIEMFKSITHSTVGSKGEKDLGASSLHVNGESLEMDSDEDDSEELEEDDGHGAEQAAAFPTEDSRTSKESMSEADRAQKMDGESEEEQESVDTGEEEEGGDESDLSSESSIKKKFLKRKGKTDSPWIKPARKRRRRSRKKPSGALGSESYKSSAGSAEQTAPGDSTGYMEVSLDSLDLRVKGILSSQAEGLANGPDVLETDGLQEVPLCSCRMETPKSREITTLANNQCMATESVDHELGRCTNSVVKYELMRPSNKAPLLVLCEDHRGRMVKHQCCPGCGYFCTAGNFMECQPESSISHRFHKDCASRVNNASYCPHCGEESSKAKEVTIAKADTTSTVTPVPGQEKGSALEGRADTTTGSAAGPPLSEDDKLQGAASHVPEGFDPTGPAGLGRPTPGLSQGPGKETLESALIALDSEKPKKLRFHPKQLYFSARQGELQKVLLMLVDGIDPNFKMEHQNKRSPLHAAAEAGHVDICHMLVQAGANIDTCSEDQRTPLMEAAENNHLEAVKYLIKAGALVDPKDAEGSTCLHLAAKKGHYEVVQYLLSNGQMDVNCQDDGGWTPMIWATEYKHVDLVKLLLSKGSDINIRDNEENICLHWAAFSGCVDIAEILLAAKCDLHAVNIHGDSPLHIAARENRYDCVVLFLSRDSDVTLKNKEGETPLQCASLNSQVWSALQMSKALQDSAPDRPSPVERIVSRDIARGYERIPIPCVNAVDSEPCPSNYKYVSQNCVTSPMNIDRNITHLQYCVCIDDCSSSNCMCGQLSMRCWYDKDGRLLPEFNMAEPPLIFECNHACSCWRNCRNRVVQNGLRARLQLYRTRDMGWGVRSLQDIPPGTFVCEYVGELISDSEADVREEDSYLFDLDNKDGEVYCIDARFYGNVSRFINHHCEPNLVPVRVFMAHQDLRFPRIAFFSTRLIEAGEQLGFDYGERFWDIKGKLFSCRCGSPKCRHSSAALAQRQASAAQEAQEDGLPDTSSAAAADPL
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
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Protein methyltransferase
Function
Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones. Also weakly methylates 'Lys-27' of histone H3 (H3K27me). Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently. Probably targeted to histone H3 by different DNA-binding proteins like E2F6, MGA, MAX and/or DP1. During G0 phase, it probably contributes to silencing of MYC- and E2F-responsive genes, suggesting a role in G0/G1 transition in cell cycle. In addition to the histone methyltransferase activity, also methylates non-histone proteins: mediates dimethylation of 'Lys-373' of p53/TP53. Represses the expression of mitochondrial function-related genes, perhaps by occupying their promoter regions, working in concert with probable chromatin reader BAZ2B (By similarity).
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Uniprot ID
Primary ID:
Q9H9B1

Secondarily ID:
B1AQ58
B1AQ59
Q86X08
Q8TCN7
Q96F53
Q96JF1
Q96KH4
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Ensembl ID
ENSG00000181090
HGNC ID
HGNC:24650
Subcellular Location
Nucleus
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0474260
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylprop-1-ynyl)quinazolin-4-amine
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C28H41N7O
  1
1
IC50 = 6 nM
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CP0467921
 Compound Info 
7-[3-(dimethylamino)propyl]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C26H43N7O
  1
1
IC50 = 9 nM
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CP0517653
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropyl)quinazolin-4-amine
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C28H45N7O
  1
1
IC50 = 9 nM
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CP0016974
 Compound Info 
5'-methoxy-6'-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3'-indole]-2'-amine
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C19H27N3O2
  1
1
IC50 = 11 nM
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CP0533829
 Compound Info 
7-[3-(dimethylamino)prop-1-ynyl]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C26H39N7O
  1
1
IC50 = 11 nM
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CP0467922
 Compound Info 
1-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]prop-2-ynyl]pyrrolidin-2-one
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C28H39N7O2
  1
1
IC50 = 12 nM
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CP0467931
 Compound Info 
2-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]propyl-methylamino]ethanol
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C27H45N7O2
  1
1
IC50 = 12 nM
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CP0046275
 Compound Info 
2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H47N5O2
  1
1
IC50 = 13 nM
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CP0474261
 Compound Info 
1-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]propyl]pyrrolidin-2-one
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C28H43N7O2
  1
1
IC50 = 16 nM
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CP0467930
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-piperidin-2-ylethyl)quinazolin-4-amine
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C28H45N7O
  1
1
IC50 = 19 nM
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CP0474249
 Compound Info 
2-cyclohexyl-7-[3-(dimethylamino)prop-1-ynyl]-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C28H41N5O
  1
1
IC50 = 19 nM
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CP0531052
 Compound Info 
2-cyclohexyl-7-[3-(dimethylamino)propyl]-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C28H45N5O
  1
1
IC50 = 19 nM
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CP0039320
 Compound Info 
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C26H43N7O2
  1
1
IC50 = 23 nM
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CP0467918
 Compound Info 
1-[3-[2-cyclohexyl-6-methoxy-4-[(1-propan-2-ylpiperidin-4-yl)amino]quinazolin-7-yl]prop-2-ynyl]pyrrolidin-2-one
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C30H41N5O2
  1
1
IC50 = 27 nM
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CP0467935
 Compound Info 
7-ethyl-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C23H36N6O
  1
1
IC50 = 35 nM
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CP0467919
 Compound Info 
7-(1-ethylpiperidin-4-yl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C28H45N7O
  1
1
IC50 = 41 nM
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CP0467915
 Compound Info 
2-cyclohexyl-6-methoxy-7-(4-methylpiperazin-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C28H44N6O
  1
1
IC50 = 44 nM
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CP0467932
 Compound Info 
7-(4-aminobut-1-ynyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C25H37N7O
  1
1
IC50 = 47 nM
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CP0474255
 Compound Info 
3-amino-N-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]propanamide
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C24H38N8O2
  1
1
IC50 = 70 nM
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CP0474258
 Compound Info 
2-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]prop-2-ynyl-methylamino]ethanol
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C27H41N7O2
  1
1
IC50 = 78 nM
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CP0519252
 Compound Info 
2-cyclohexyl-6-fluoro-7-(4-methylpiperazin-1-yl)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C27H41FN6
  1
1
IC50 = 94 nM
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CP0538107
 Compound Info 
5-amino-N-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]pentanamide
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C26H42N8O2
  1
1
IC50 = 122 nM
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CP0519256
 Compound Info 
3-(dimethylamino)-N-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]propanamide
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C26H42N8O2
  1
1
IC50 = 150 nM
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CP0529734
 Compound Info 
6-methoxy-7-[3-(methylamino)prop-1-ynyl]-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C25H37N7O
  1
1
IC50 = 152 nM
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CP0545901
 Compound Info 
7-(3-aminopropyl)-2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C26H41N5O
  1
1
IC50 = 179 nM
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CP0517652
 Compound Info 
1-[3-[2-cyclohexyl-6-methoxy-4-[(1-propan-2-ylpiperidin-4-yl)amino]quinazolin-7-yl]propyl]pyrrolidin-2-one
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C30H45N5O2
  1
1
IC50 = 205 nM
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CP0531054
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-propylquinazolin-4-amine
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C24H38N6O
  1
1
IC50 = 280 nM
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CP0467929
 Compound Info 
1-(3-aminopropyl)-3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]urea
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C25H41N9O2
  1
1
IC50 = 300 nM
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CP0474257
 Compound Info 
N-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]propyl]acetamide
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C26H41N7O2
  1
1
IC50 = 529 nM
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CP0467924
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazoline-7-carboxamide
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C22H33N7O2
  1
1
IC50 = 642 nM
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CP0531056
 Compound Info 
2-cyclohexyl-7-[3-(dimethylamino)propyl]-6-ethoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C29H47N5O
  1
1
IC50 = 647 nM
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CP0519253
 Compound Info 
7-(3-aminoprop-1-ynyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C24H35N7O
  1
1
IC50 = 679 nM
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CP0474259
 Compound Info 
N-[3-[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]prop-2-ynyl]acetamide
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C26H37N7O2
  1
1
IC50 = 698 nM
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CP0551657
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-piperidin-4-ylethyl)quinazolin-4-amine
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C28H45N7O
  1
1
IC50 = 885 nM
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CP0557887
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C21H32N6O
  1
1
IC50 = 926 nM
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CP0533828
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-pyridin-2-ylquinazolin-4-amine
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C26H35N7O
  1
1
IC50 = 953 nM
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CP0561857
 Compound Info 
7-(3-aminopropyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C24H39N7O
  1
1
IC50 = 1080 nM
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CP0531055
 Compound Info 
2-cyclohexyl-6-methoxy-7-piperidin-4-yl-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C28H43N5O
  1
1
IC50 = 1250 nM
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CP0467926
 Compound Info 
2-cyclohexyl-7-[3-(dimethylamino)propyl]-6-fluoro-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C27H42FN5
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1
IC50 = 1310 nM
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CP0551655
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-pyridin-2-ylethyl)quinazolin-4-amine
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C28H39N7O
  1
1
IC50 = 1350 nM
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CP0467927
 Compound Info 
7-(3-aminopropyl)-2-cyclohexyl-6-fluoro-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C25H38FN5
  1
1
IC50 = 1460 nM
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CP0545902
 Compound Info 
7-(3-aminoprop-1-ynyl)-2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C26H37N5O
  1
1
IC50 = 1550 nM
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CP0538105
 Compound Info 
2-cyclohexyl-7-[3-(dimethylamino)prop-1-ynyl]-6-ethoxy-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C29H43N5O
  1
1
IC50 = 1950 nM
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CP0467928
 Compound Info 
7-(3-aminoprop-1-ynyl)-2-cyclohexyl-6-fluoro-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C25H34FN5
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1
IC50 = 2010 nM
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CP0519259
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-piperidin-3-ylquinazolin-4-amine
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C26H41N7O
  1
1
IC50 = 2230 nM
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CP0474253
 Compound Info 
2-cyclohexyl-6-methoxy-7-(3-morpholin-4-ylpropyl)-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C30H47N5O2
  1
1
IC50 = 2360 nM
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CP0467920
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-phenylquinazolin-4-amine
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C27H36N6O
  1
1
IC50 = 2380 nM
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CP0519258
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-pyridin-3-ylquinazolin-4-amine
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C26H35N7O
  1
1
IC50 = 2470 nM
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CP0519257
 Compound Info 
N-(2-aminoethyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazoline-7-carboxamide
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C24H38N8O2
  1
1
IC50 = 2650 nM
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CP0467933
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]-N-(4-pyrrolidin-1-ylbutyl)quinazoline-7-carboxamide
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C30H48N8O2
  1
1
IC50 = 2860 nM
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CP0531053
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-piperidin-2-ylquinazolin-4-amine
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C26H41N7O
  1
1
IC50 = 3090 nM
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CP0474252
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-pyridin-2-ylethynyl)quinazolin-4-amine
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C28H35N7O
  1
1
IC50 = 3470 nM
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CP0467913
 Compound Info 
2-cyclohexyl-7-N-[2-(dimethylamino)ethyl]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)quinazoline-4,7-diamine
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C27H44N6O
  1
1
IC50 = 3990 nM
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CP0531057
 Compound Info 
N-(4-aminobutyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazoline-7-carboxamide
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C26H42N8O2
  1
1
IC50 = 4090 nM
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CP0467917
 Compound Info 
6-chloro-2-cyclohexyl-7-[3-(dimethylamino)propyl]-N-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine
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C27H42ClN5
  1
1
IC50 = 4670 nM
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CP0474262
 Compound Info 
N-(3-aminopropyl)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazoline-7-carboxamide
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C25H40N8O2
  1
1
IC50 = 7510 nM
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CP0474256
 Compound Info 
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-pyridin-4-ylquinazolin-4-amine
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C26H35N7O
  1
1
IC50 = 10300 nM
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CP0467923
 Compound Info 
N-[2-(dimethylamino)ethyl]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazoline-7-carboxamide
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C26H42N8O2
  1
1
IC50 = 18500 nM
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CP0529721
 Compound Info 
[6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-[(1-methylpiperidin-4-yl)amino]quinazolin-7-yl]-piperazin-1-ylmethanone
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C26H40N8O2
  1
1
IC50 = 53600 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0046275
 Compound Info 
2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
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C30H47N5O2
  1
1 IC50 = 19 nM
CP0039320
 Compound Info 
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C26H43N7O2
  3
1 IC50 = 20 nM
2 IC50 = 50 nM
3 IC50 = 58 nM
CP0016974
 Compound Info 
5'-methoxy-6'-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3'-indole]-2'-amine
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C19H27N3O2
  2
1 IC50 = 38 nM
2 IC50 = 118.1 nM
Clinical Information about the Protein
Target 1 ( Euchromatic histone-lysine N-methyltransferase 1 (EHMT1) )
Target Type Literature-reported Target
Disease 2 Target-related Diseases  2
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Breast cancer [ICD-11: 2C60-2C65]
Preclinical Drug(s) 2 Preclinical Drugs  2
1 A-366
 Drug Info 
Preclinical
Solid tumour/cancer
2 BIX-01294
 Drug Info 
Preclinical
Breast cancer