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Title | Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. |
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Journal, issue, pages | J. Med. Chem., Vol. 61, Page 10155-10172, Year 2018 |
Publish date | Aug 17, 2018 (structure data deposition date) |
Authors | Papillon, J.P.N. / Nakajima, K. / Adair, C.D. / Hempel, J. / Jouk, A.O. / Karki, R.G. / Mathieu, S. / Mobitz, H. / Ntaganda, R. / Smith, T. ...Papillon, J.P.N. / Nakajima, K. / Adair, C.D. / Hempel, J. / Jouk, A.O. / Karki, R.G. / Mathieu, S. / Mobitz, H. / Ntaganda, R. / Smith, T. / Visser, M. / Hill, S.E. / Hurtado, F.K. / Chenail, G. / Bhang, H.C. / Bric, A. / Xiang, K. / Bushold, G. / Gilbert, T. / Vattay, A. / Dooley, J. / Costa, E.A. / Park, I. / Li, A. / Farley, D. / Lounkine, E. / Yue, Q.K. / Xie, X. / Zhu, X. / Kulathila, R. / King, D. / Hu, T. / Vulic, K. / Cantwell, J. / Luu, C. / Jagani, Z. |
External links | J. Med. Chem. / PubMed:30339381 |
Methods | X-ray diffraction |
Resolution | 2.84 - 2.98 Å |
Structure data | PDB-6eg2: PDB-6eg3: |
Chemicals | ChemComp-J7J: ChemComp-IPA: ChemComp-HOH: ChemComp-J7G: ChemComp-EOH: |
Source |
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Keywords | Hydrolase/Hydrolase Inhibitor / Helicase / ATPase / Chromatin remodeling / inhibitor / MBP fusion / Hydrolase-Hydrolase Inhibitor complex |