Identification of Triazolopyridines as Selective α5-GABA A Receptor Negative Allosteric Modulators by a Hybridization Approach


ACS Chem. Neurosci, 14, 148–158.


Szabó, G., Károlyi, B. I., Gnes, A. ́, Vaskó, G., Potor, A., Vukics, K., Kapus, G. L., Fodor, L., Bobok, A., Vastag, M., & Bata, I.



The identification and characterization of novel triazolopyridine derivatives with selective α5 subunit-containing GABA A receptor negative allosteric modulator (NAM) activity are disclosed. As a result of in silico screening of our corporate compound deck, we identified a moderately potent hit that was converted to an advanced hit bearing better physicochemical and pharmacological properties using a hybridization approach. Subsequent optimization led to the identification of in vitro potent and subtype-selective α5-GABA A receptor NAMs representing a new chemotype in this area.

Go to journal

Get in Touch

We strive to provide the best for our customers, and we are always ready to help. Please let us know if you have a question for us.

Follow us