Target Poor or Non Binder(s) Information

Target General Information

Target ID

T39519

Target Info

Target Name

Lysine N-methyltransferase 1A (SUV39H1)

Synonyms

Suppressor of variegation 3-9 homolog 1; Su(var)3-9 homolog 1; SUV39H; Position-effect variegation 3-9 homolog; KMT1A; Histone-lysine N-methyltransferase SUV39H1; Histone H3-K9 methyltransferase 1; H3-K9-HMTase 1

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Target Type

Literature-reported Target

Gene Name

SUV39H1

Biochemical Class

Methyltransferase

UniProt ID

O43463

Poor Binders of This Target (in total, 14 binders)

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Compound Name

GSK343

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Investigative

Compound Info

Synonyms

compound 6 [PMID 24900432]; GSK 343

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

1-[3-[[(1S,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea

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Investigative

Compound Info

Synonyms

CHEMBL3087501; SCHEMBL16424780; BDBM50443020

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Activity

Ki ~ 50000 nM

[2]

Compound Name

1-[3-[[(1R,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea

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Investigative

Compound Info

Synonyms

CHEMBL3087503; SCHEMBL16424848; BDBM50443018

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Activity

Ki ~ 50000 nM

[2]

Compound Name

1-[3-[[(3R,4S,5R)-3-(6-Aminopurin-9-yl)-4,5-dihydroxycyclopenten-1-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea

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Investigative

Compound Info

Synonyms

CHEMBL3087502; SCHEMBL16424776; BDBM50443019

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Activity

Ki ~ 50000 nM

[2]

Compound Name

5'-[(3-{[(4-Tert-Butylphenyl)carbamoyl]amino}propyl)(Propan-2-Yl)amino]-5'-Deoxyadenosine

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Investigative

Compound Info

Synonyms

CHEMBL2171169; SCHEMBL9970132; BDBM50396980; ZINC95557720; Q27458098

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Activity

Ki ~ 50000 nM

[2]

Compound Name

(2S)-2-Amino-5-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL2172427; BDBM50396017

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Activity

IC50 ~ 100000 nM

[3]

Compound Name

(2s)-2-Azanyl-4-[[(2s,3s,4r,5r)-5-[6-(Methylamino)purin-9-Yl]-3,4-Bis(Oxidanyl)oxolan-2-Yl]methylsulfanyl]butanoic Acid

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Investigative

Compound Info

Synonyms

CHEMBL2171174; Methyl-SAH; SCHEMBL9058595; BDBM50396981; S-(N6-Methyladenosyl)-L-homocysteine; Q27466742

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Activity

Ki ~ 100000 nM

[4]

Compound Name

(2S)-2-Amino-5-[[(2R,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL2169918; BDBM50396016

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Activity

IC50 ~ 100000 nM

[3]

Compound Name

N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indazole-4-carboxamide

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Investigative

Compound Info

Synonyms

GSK926; CHEMBL2204998; SCHEMBL2590353; BDBM50400779

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(prop-2-enylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]urea

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Investigative

Compound Info

Synonyms

CHEMBL2171171; BDBM50396978

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Activity

Ki ~ 100000 nM

[4]

Compound Name

1-[3-[[(2R,3S,4R,5R)-5-[6-(Benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea

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Investigative

Compound Info

Synonyms

CHEMBL2171172; BDBM50396977

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Activity

Ki ~ 100000 nM

[4]

Compound Name

1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]urea

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Investigative

Compound Info

Synonyms

CHEMBL2171170; BDBM50396979

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Activity

Ki ~ 100000 nM

[4]

Compound Name

N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL2204997; SCHEMBL12180659; BDBM50400781

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

1-((2-(1H-Indol-3-yl)ethyl)amino)-3-(9H-carbazol-9-yl)-propan-2-ol

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Investigative

Compound Info

Synonyms

DC_05; DC-05; CHEMBL3358015; C25H25N3O; AOB6967; SYN5082; BDBM50031317; AKOS002242638; AKOS016316322; NCGC00402253-02; AS-16448; DC_05, >=98% (HPLC); HY-12746; ST50753266; 1-carbazol-9-yl-3-[(2-indol-3-ylethyl)amino]propan-2-ol; 1-carbazol-9-yl-3-[2-(1H-indol-3-yl)ethylamino]propan-2-ol; 1-(9H-Carbazole-9-yl)-3-[[2-(1H-indole-3-yl)ethyl]amino]-2-propanol

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Activity

IC50 ~ 150000 nM

[5]

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References

Top

REF 1

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.

REF 2

Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L. Medchemcomm. 2013 May 1;4(5):822-826.

REF 3

Oncoepigenomics: making histone lysine methylation count. Eur J Med Chem. 2012 Oct;56:179-94.

REF 4

Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L. J Med Chem. 2012 Sep 27;55(18):8066-74.

REF 5

Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-41.

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