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. Author manuscript; available in PMC: 2012 Aug 17.
Published in final edited form as: ACS Chem Neurosci. 2011 Aug 17;2(8):411–432. doi: 10.1021/cn2000266

Table 13.

mGlu5 potency and intrinsic clearance in 2-benzimidazolyl analogues

graphic file with name nihms-291053-t0012.jpg

Entry R1 R2 R3 R4 R5 mGlu5 IC50 (nM) Rat ClINT (μL/min/mg) Human ClINT (μL/min/mg)
186 nPr H H H H 100 83 158
187 Et H H H H 110 120 118
188 nBu H H H H 360 347 279
189 iBu H H H H 110 55 826
190 nPr Cl H H H 200 74 69
191 nPr H Cl H H > 500 400 34
192 nPr H H Cl H 130 56 33
193 nPr H H H Cl 24 83 112