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

Table 6. mGlu5 Potency and Protein Binding in the Thiazolotriazole Series.

graphic file with name cn-2011-000266_0017.jpg

entry R1 R2 R3 R4 mGlu5 IC50 (nM) fub pIC50 eff
82 H H H phenyl >30 000    
83 H Me H phenyl >30 000    
84 H H Me phenyl 10 000    
85 H Me Me phenyl 63 6.8 6.0
86 H Me Me cyclohexyl 3200    
87 H Me Me 3-chlorophenyl 40 0.9 5.4
88 H Me Me 3-fluorophenyl 50 1.7 5.5
89 H Me Me 3-pyridyl 316 28 5.9
90 cyclopropyl Me Me phenyl 13    
91 thiophen-2-yl Me Me phenyl 7.9 <0.1 <5.0