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TitleDevelopment of Dimethylisoxazole-Attached Imidazo[1,2- a ]pyridines as Potent and Selective CBP/P300 Inhibitors.
Journal, issue, pagesJ. Med. Chem., Vol. 64, Page 5787-5801, Year 2021
Publish dateNov 12, 2020 (structure data deposition date)
AuthorsMuthengi, A. / Wimalasena, V.K. / Yosief, H.O. / Bikowitz, M.J. / Sigua, L.H. / Wang, T. / Li, D. / Gaieb, Z. / Dhawan, G. / Liu, S. ...Muthengi, A. / Wimalasena, V.K. / Yosief, H.O. / Bikowitz, M.J. / Sigua, L.H. / Wang, T. / Li, D. / Gaieb, Z. / Dhawan, G. / Liu, S. / Erickson, J. / Amaro, R.E. / Schonbrunn, E. / Qi, J. / Zhang, W.
External linksJ. Med. Chem. / PubMed:33872011
MethodsX-ray diffraction
Resolution1.7 Å
Structure data

PDB-7kpy:
Crystal structure of CBP bromodomain liganded with UMB298 (compound 23)
Method: X-RAY DIFFRACTION / Resolution: 1.7 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-WU1:
2-[2-(3-chloranyl-4-methoxy-phenyl)ethyl]-~{N}-cyclohexyl-7-(3,5-dimethyl-1,2-oxazol-4-yl)imidazo[1,2-a]pyridin-3-amine

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / epigenetics / inhibitor / drug development / multi domain proteins

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