TABLE 3 

ZINC Compounds identified by virtual screening and tested for activity

IPYD/IControl Mean ± S.E.M. %EC50μM (%)aIPYD/IControl
Mean ± S.E.M. %EC50μM (%)aμM (%)a
GluN2AGluN2BGluN2CGluN2DGluN2CGluN2AGluN2BGluN2CGluN2DGluN2C
181cEmbedded Image100 ± 1.596 ± 0.61114 ± 2.399 ± 1.1N.D. (130)187bEmbedded Image97 ± 1.895 ± 2.697 ± 1.494 ± 0.82N.D.
182cEmbedded Image96 ± 1.396 ± 0.93108 ± 2.497 ± 0.70N.D. (114)188bEmbedded Image95 ± 1.792 ± 1.989 ± 1.289 ± 0.86N.D.
183cEmbedded Image99 ± 4.296 ± 2.1120 ± 2.283 ± 0.84N.D. (115)189bEmbedded Image97 ± 0.5694 ± 1.593 ± 0.4591 ± 0.90N.D.
184cEmbedded Image92 ± 3.991 ± 1.9134 ± 4.1103 ± 6.19 (132)190dEmbedded Image96 ± 6.265 ± 1.071 ± 0.2767 ± 0.78N.D.
185dEmbedded Image97 ± 1.590 ± 1.593 ± 0.9676 ± 2.2N.D.191bEmbedded Image94 ± 1.694 ± 4.290 ± 1.490 ± 0.41N.D.
186dEmbedded Image76 ± 5.255 ± 4.548 ± 2.536 ± 1.9N.D.192cEmbedded Image100 ± 6.990 ± 0.9985 ± 0.3784 ± 0.52N.D.
  • All compounds were coapplied with 100 glutamate and 30 μM glycine. The concentration-effect curve was recorded for active compounds and fitted by the Hill equation (see Materials and Methods) to determine the EC50 value; parentheses show the response to 100 μM test compound as a percentage of the response to maximally effective concentrations of glutamate (100 μM) and glycine (30 μM) for compounds tested at multiple concentrations. Compounds were screened at b10 μM, c30 μM, and d100 μM depending on availability and solubility. N.D., not determined. For all compounds, data are from three to 12 oocytes from one to three different frogs.