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. 2011 Apr 15;2(8):411–432. doi: 10.1021/cn2000266

Table 12. mGlu5 Potency, Solubility, and Intrinsic Clearance in the Nicotinamide Series.

graphic file with name cn-2011-000266_0032.jpg

entry R1 R2 mGlu5 IC50 (nM) solubility at pH 6.8 (mg/mL) rat ClINT (μL/min/mg) human ClINT (μL/min/mg)
181 H H 87 150 48 33
(R)-182 H R-ethyl 40 95 643 322
(S)-182 H S-ethyl 40 <3 687 174
(R)-183 R-ethyl H 32 58 87 89
(S)-183 S-ethyl H 390 56 190 216