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Title | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. |
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Journal, issue, pages | Bioorg. Med. Chem., Vol. 26, Page 2937-2957, Year 2018 |
Publish date | Feb 20, 2018 (structure data deposition date) |
![]() | Jennings, L.E. / Schiedel, M. / Hewings, D.S. / Picaud, S. / Laurin, C.M.C. / Bruno, P.A. / Bluck, J.P. / Scorah, A.R. / See, L. / Reynolds, J.K. ...Jennings, L.E. / Schiedel, M. / Hewings, D.S. / Picaud, S. / Laurin, C.M.C. / Bruno, P.A. / Bluck, J.P. / Scorah, A.R. / See, L. / Reynolds, J.K. / Moroglu, M. / Mistry, I.N. / Hicks, A. / Guzanov, P. / Clayton, J. / Evans, C.N.G. / Stazi, G. / Biggin, P.C. / Mapp, A.K. / Hammond, E.M. / Humphreys, P.G. / Filippakopoulos, P. / Conway, S.J. |
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Methods | X-ray diffraction |
Resolution | 1.28 - 1.34 Å |
Structure data | ![]() PDB-6fsy: ![]() PDB-6ft3: ![]() PDB-6ft4: |
Chemicals | ![]() ChemComp-EDO: ![]() ChemComp-E5Q: ![]() ChemComp-HOH: ![]() ChemComp-E5T: ![]() ChemComp-E5W: |
Source |
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![]() | TRANSCRIPTION / Bromodomain / ligand / isoxazole / Structural Genomics / Structural Genomics Consortium / SGC |