Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM1H45U)

Drug Name

A-366 Drug Info

Synonyms

A 366; A366

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Preclinical	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Preclinical Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Euchromatic histone-lysine N-methyltransferase 1 (EHMT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIX-01294	DM5CBNY	Breast cancer	2C60-2C65	Preclinical	[3]
UNC0642	DM7Y1SO	Discovery agent	N.A.	Investigative	[4]
UNC0638	DM4A1KJ	Discovery agent	N.A.	Investigative	[5]
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Drug(s) Targeting Histone-lysine N-methyltransferase EHMT2 (EHMT2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIX-01294	DM5CBNY	Breast cancer	2C60-2C65	Preclinical	[3]
MS012	DM5AMFV	Inflammation	1A00-CA43.1	Preclinical	[1]
UNC0642	DM7Y1SO	Discovery agent	N.A.	Investigative	[4]
UNC0638	DM4A1KJ	Discovery agent	N.A.	Investigative	[5]
UNC0321	DMCVU1T	Discovery agent	N.A.	Investigative	[6]
BRD9539	DMFAVB5	Discovery agent	N.A.	Investigative	[7]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Euchromatic histone-lysine N-methyltransferase 1 (EHMT1)	TTOFXD7	EHMT1_HUMAN	Inhibitor	[2]
Histone-lysine N-methyltransferase EHMT2 (EHMT2)	TTS6RZT	EHMT2_HUMAN	Inhibitor	[2]

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References

1	Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
2	Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9.
3	Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.
4	Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42.
5	A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.
6	Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57.
7	A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.