GPCRs are now the target of about 40 % of all drugs, demonstrating their enormous importance in drug design. Elucidating the function and the activation of the remaining orphan GPCRs is therefor of enormous importance. The adhesion GPCRs (aGPCRs) form the most enigmatic group of GPCRs at present. My work focuses on the development of biological active compounds for the GPR114. This is done cooperatively as an iterative cycle of GPCR modelling, my synthesis and the biological evaluation.