5KTX
CREBBP bromodomain in complex with Cpd59 ((S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)ethanone)
Summary for 5KTX
Entry DOI | 10.2210/pdb5ktx/pdb |
Related | 5KTW 5KU3 |
Descriptor | CREB-binding protein, 1-[3-[[2-fluoranyl-4-(1-methylpyrazol-4-yl)phenyl]amino]-1-[(3~{S})-oxolan-3-yl]-6,7-dihydro-4~{H}-pyrazolo[4,3-c]pyridin-5-yl]ethanone, 1,2-ETHANEDIOL, ... (5 entities in total) |
Functional Keywords | crebbp bromodomain, transferase |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm: Q92793 |
Total number of polymer chains | 1 |
Total formula weight | 14172.21 |
Authors | Murray, J.M.,Noland, C. (deposition date: 2016-07-12, release date: 2016-11-02, Last modification date: 2024-03-06) |
Primary citation | Crawford, T.D.,Romero, F.A.,Lai, K.W.,Tsui, V.,Taylor, A.M.,de Leon Boenig, G.,Noland, C.L.,Murray, J.,Ly, J.,Choo, E.F.,Hunsaker, T.L.,Chan, E.W.,Merchant, M.,Kharbanda, S.,Gascoigne, K.E.,Kaufman, S.,Beresini, M.H.,Liao, J.,Liu, W.,Chen, K.X.,Chen, Z.,Conery, A.R.,Cote, A.,Jayaram, H.,Jiang, Y.,Kiefer, J.R.,Kleinheinz, T.,Li, Y.,Maher, J.,Pardo, E.,Poy, F.,Spillane, K.L.,Wang, F.,Wang, J.,Wei, X.,Xu, Z.,Xu, Z.,Yen, I.,Zawadzke, L.,Zhu, X.,Bellon, S.,Cummings, R.,Cochran, A.G.,Albrecht, B.K.,Magnuson, S. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J. Med. Chem., 59:10549-10563, 2016 Cited by PubMed: 27682507DOI: 10.1021/acs.jmedchem.6b01022 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.27 Å) |
Structure validation
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