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(A) The three regions of compounds 1 (R = OMe) and 4 (R = H). (B) X-ray crystal structure of compound 1 (carbon = yellow) bound to the CREBBP bromodomain (PDB code: 4NYX). The dihydroquinoxalinone headgroup binds to the KAc pocket forming hydrogen bonding interactions with N1168. (C) The electron-rich 7-(methoxy)tetrahydroquinoline group of 1 forms cation−π interactions with the positively charged R1173.11
