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. Author manuscript; available in PMC: 2015 Aug 1.
Published in final edited form as: Bioorg Med Chem Lett. 2014 Jun 11;24(15):3307–3314. doi: 10.1016/j.bmcl.2014.06.003

Table 3. Heteroaryl Amide SAR.

graphic file with name nihms-607969-t0016.jpg

Cpd A R mGlu5
pIC50a
(± SEM)
mGlu5
IC50
(nM)
% Glu
Maxa,b
(± SEM)
51 N graphic file with name nihms-607969-t0017.jpg <5.0c >10,000 20d
52 N graphic file with name nihms-607969-t0018.jpg <5.0c >10,000 15 ± 8
53 N graphic file with name nihms-607969-t0019.jpg <5.0c >10,000 35 ± 6
54 CF graphic file with name nihms-607969-t0020.jpg 5.2 ± 0.11 6370 7.8 ± 2.8
55 CF graphic file with name nihms-607969-t0021.jpg 5.5 ± 0.15 3450 0.1 ± 2.4
56 CF graphic file with name nihms-607969-t0022.jpg <4.5 >30,000
57 CF graphic file with name nihms-607969-t0023.jpg <5.0c >10,000 40 ± 9
58 CF graphic file with name nihms-607969-t0024.jpg 5.07 ± 0.05 8430 22 ± 11
59 CF graphic file with name nihms-607969-t0025.jpg <5.0c >10,000 40 ± 15
60 CF graphic file with name nihms-607969-t0026.jpg <4.5 >30,000
61 CF graphic file with name nihms-607969-t0027.jpg <4.5 >30,000
62 CF graphic file with name nihms-607969-t0028.jpg <4.5 >30,000
63 CF graphic file with name nihms-607969-t0029.jpg <4.5 >30,000
64 CF graphic file with name nihms-607969-t0030.jpg <4.5 >30,000
a

Calcium mobilization mGlu5 assay; values are average of n ≥ 3

b

Amplitude of response in the presence of 30 μM test compound as a percentage of maximal response (100 μM glutamate); average of n ≥ 3

c

CRC does not plateau

d

average of n = 2