Type A γ-aminobutyric acid (GABAA) receptors are pentameric ligand-gated chloride channels and serves as the main drivers of fast inhibitory neurotransmission in the vertebrate nervous system. 1,2 Dysfunction of GABAA receptors is implicated in a range of neurological disorders, including schizophrenia, autism, and epilepsy3,4,5.We’re presenting the building of in silico models based on a comprehensive and high-quality dataset set generated by Saniona A/S, Denmark. These models were utilized in an innovative computational and medicinal chemistry strategy. This novel approach allowed a drastic reduction of the number of molecules prepared and accelerated the Design Make Test Analyse (DMTA) cycle, which led to the discovery of an advanced, selective, and potent drug candidate for CNS diseases.As part of our commitment to the scientific community, one of our compounds will be presented and is made available on the opnMe.com platform for researchers to utilize. This initiative aims to foster collaboration and accelerate progress in CNS disease research.Sigel, E. & Steinmann, M. E., J. Biol. Chem. 2012, 287, 40224Olsen, R. W. & Sieghart, W., Neuropharmacology, 2009, 56, 141Braat, S. & Kooy, R. F. Neuron, 2015, 86, 1119Macdonald, R. L., Kang, J.-Q. & Gallagher, M. J., J. Physiol, 2010,588, 1861Jacob, T. C., Front. Mol. Neurosci. 2019, 12: 179