Substance use disorder remains a major, unmet medical need. Cocaine is one of the most commonly abused recreational drugs and in 2018, there were over 5.5 million current cocaine users. There are no approved therapies for the treatment of cocaine use disorder, but the D3 dopamine receptor has been identified as a potential therapeutic target. We have identified a series of functionalized diamino-butylbenzamides that are potent D3 binders with moderate to high selectivity for D3 over D2.