The potential effectiveness of 5-HT6 receptor active agents as cognitive enhancers has been the focal point of research in Alzheimer’s disease (AD). Serotonin 5-HT6 receptors are distributed in brain regions affiliated with memory and learning making them promising, novel targets for (CNS)-mediated diseases such as Alzheimer's disease (cognitive function). A group of previously reported compounds was selected and tested in vitro for the binding affinity to 5-HT6 receptors. The binding affinity of these compounds was tested using in vitro radioligand binding assay using cryopreserved membrane expressing target receptors as grounds for the assay and the use of Methiothepin and Haloperidol as references. Data was analyzed by calculating the total binding percentage, which was performed for the references and tested compounds. It was found that the tested compounds displayed promising activity as 5-HT6 antagonists and partial dopamine 2 agonists. The binding mode of tested compounds was studied by molecular docking using SB-271046 as reference. The tested compounds binds with Arg 86 and Lys 14 aminoacid residues which proves the rationality of the developed models. These results may be helpful in designing novel and potential 5-HT6 ligands.