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TitleDiscovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
Journal, issue, pagesJ. Med. Chem., Vol. 52, Page 7950-7953, Year 2009
Publish dateOct 7, 2009 (structure data deposition date)
AuthorsLiu, F. / Chen, X. / Allali-Hassani, A. / Quinn, A.M. / Wasney, G.A. / Dong, A. / Barsyte, D. / Kozieradzki, I. / Senisterra, G. / Chau, I. ...Liu, F. / Chen, X. / Allali-Hassani, A. / Quinn, A.M. / Wasney, G.A. / Dong, A. / Barsyte, D. / Kozieradzki, I. / Senisterra, G. / Chau, I. / Siarheyeva, A. / Kireev, D.B. / Jadhav, A. / Herold, J.M. / Frye, S.V. / Arrowsmith, C.H. / Brown, P.J. / Simeonov, A. / Vedadi, M. / Jin, J.
External linksJ. Med. Chem. / PubMed:19891491
MethodsX-ray diffraction
Resolution1.7 Å
Structure data

PDB-3k5k:
Discovery of a 2,4-Diamino-7-aminoalkoxy-quinazoline as a Potent Inhibitor of Histone Lysine Methyltransferase, G9a
Method: X-RAY DIFFRACTION / Resolution: 1.7 Å

Chemicals

ChemComp-ZN:
Unknown entry

ChemComp-SAH:
S-ADENOSYL-L-HOMOCYSTEINE

ChemComp-DXQ:
7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine

ChemComp-CL:
Unknown entry

ChemComp-UNX:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Histone Lysine Methyltransferase / G9A / ANK repeat / Chromatin regulator / Metal-binding / Methyltransferase / Nucleus / Phosphoprotein / S-adenosyl-L-methionine / Structural Genomics / Structural Genomics Consortium / SGC

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