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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 6.

mGlu5 potency and protein binding in the thiazolotriazole series

graphic file with name nihms-291053-t0006.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