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. 2019 Jan 4;10(3):248–254. doi: 10.1021/acsmedchemlett.8b00395

Table 3. Comparison of Sulfonamide to Amide Linkera.

      Idrug/Icontrol (mean ± SEM, %)b, IC50 (μM)c
Cmpd # cLogPd Drug μM GluN2A GluN2C GluN2D
9 3.55 6 5.1 ± 1.3 ND ND
0.17
26 4.22 30 102 ± 2.2 ND ND
ND
23 4.34 30 85 ± 1.2 9.0 ± 2.8 8.9 ± 2.3
ND 2.4 1.7
27 4.59 30 82 ± 8.6 56 ± 1.9 49 ± 1.6
ND 37 29
a

Data are from 8 to 9 oocytes from 2 frogs for each compound tested.

b

The response to drug coapplied with a maximally effective concentration of glutamate (100 μM) and glycine (30 μM) is given as a percent of the control response to glutamate and glycine alone.

c

IC50 values were determined by fitting the Hill equation to the average composite concentration–response curve and are reported to two significant figures. ND indicates not determined.

d

cLogP calculated using Chemicalize from ChemAxon.