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TitleDiscovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.
Journal, issue, pagesEur J Med Chem, Vol. 147, Page 238-252, Year 2018
Publish dateJul 4, 2017 (structure data deposition date)
AuthorsXiang, Q. / Wang, C. / Zhang, Y. / Xue, X. / Song, M. / Zhang, C. / Li, C. / Wu, C. / Li, K. / Hui, X. ...Xiang, Q. / Wang, C. / Zhang, Y. / Xue, X. / Song, M. / Zhang, C. / Li, C. / Wu, C. / Li, K. / Hui, X. / Zhou, Y. / Smaill, J.B. / Patterson, A.V. / Wu, D. / Ding, K. / Xu, Y.
External linksEur J Med Chem / PubMed:29448139
MethodsX-ray diffraction
Resolution1.62 Å
Structure data

PDB-5xxh:
Crystal Structure Analysis of the CBP
Method: X-RAY DIFFRACTION / Resolution: 1.62 Å

Chemicals

ChemComp-E0D:
(3S)-1-[2-(3-ethanoylindol-1-yl)ethanoyl]piperidine-3-carboxylic acid

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-MG:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / CBP / Bromodomain

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