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TitleOptimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
Journal, issue, pagesMedchemcomm, Vol. 5, Page 1879-1886, Year 2014
Publish dateJun 27, 2014 (structure data deposition date)
AuthorsEngland, K.S. / Tumber, A. / Krojer, T. / Scozzafava, G. / Ng, S.S. / Daniel, M. / Szykowska, A. / Che, K. / von Delft, F. / Burgess-Brown, N.A. ...England, K.S. / Tumber, A. / Krojer, T. / Scozzafava, G. / Ng, S.S. / Daniel, M. / Szykowska, A. / Che, K. / von Delft, F. / Burgess-Brown, N.A. / Kawamura, A. / Schofield, C.J. / Brennan, P.E.
External linksMedchemcomm / PubMed:26682034
MethodsX-ray diffraction
Resolution2.23 Å
Structure data

PDB-4ura:
Crystal structure of human JMJD2A in complex with compound 14a
Method: X-RAY DIFFRACTION / Resolution: 2.23 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-SO4:
SULFATE ION

ChemComp-NI:
NICKEL (II) ION

ChemComp-ZN:
Unknown entry

ChemComp-LEL:
2-(2H-1,2,3-triazol-4-yl)pyridine-4-carboxylic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / JUMONJIC / HISTONE DEMETHYLASE

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