Herein, we present the results of the study devoted to the exploration of BSA binding of 2-(aminomethyl)cyclopropane-1,1-dicarboxylic acid, as an example of constrained γ-amino dicarboxylic acid, and, taking into consideration that the effectiveness of a potential drug depends on its ability to bind to a protein carrier and in that way enable transfer through the blood stream. For the investigation of binding properties, we used the fluorescence emission titration of BSA with a synthesized compound. Considering that the BSA solution shows an intensive fluorescence emission around 360 nm, a decrease in emission intensity at λ = 366 nm with the addition of a solution of 2-(aminomethyl)cyclopropane-1,1-dicarboxylic acid indicated the binding of the tested compound. According to the results obtained, our compound binds to the BSA in a molar ratio 1:1 (n ≈ 1). The optimal values of binding constant Ka are between 104 and 106 M−1, which indicates to us that the Ka value of the tested compound is in the favorable range.