Background and Purpose. New psychoactive substances (NPSs) often emerge on the illicit drug market with limited pharmacological or toxicological data. Synthetic cathinones are the second largest NPS group, often mimicking the effects of classical stimulants such as cocaine and MDMA. Such stimulants primarily target dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters, with DAT selectivity being linked to abuse potential. Due to the lack of pharmacological profiling, this study aimed to determine the potencies and structure-activity relationships (SARs) of recently emerged stimulants. Experimental Approach. Employing in vitro human transporter inhibition assay and AequoScreen® 5HT 2A receptor activity assay, potency, transporter selectivity, DAT/SERT, DAT/NET, and NET/SERT ratios, and group-wide structure-activity relationships of 58 substances were investigated. Key Results. Most synthetic cathinones inhibited DAT at nanomolar concentrations, with N-pyrrolidine cathinones in combination with methylenedioxy groups – MDPiHP, MDPEP, and MDPV – demonstrating the highest DAT potency among all the tested stimulants. In contrast, other N-pyrrolidine cathinones, 3F-α-PHP, 3F-α-PiHP, and 4F-α-PiHP exhibited the highest DAT selectivity (DAT/SERT ratio). CMC and MMC compounds, such as 3-CMC, exhibited a distinct amphetamine-like pharmacological profile showing a comparable potency between DAT and NET. Some cathinones at high concentrations and phenethylamines in micromolar concentrations additionally activated the 5HT 2A receptor, while 2C-like arylcyclohexylamines primarily targeted the receptor without transporter inhibition. Conclusion and Implications. These results show that cathinones displayed distinct group SARs. Based on the DAT/SERT selectivity, the majority of the investigated compounds, especially N-pyrrolidine cathinones, suggest a high abuse potential.