Table 5. Comparison of mGlu1 NAM Activitya with Affinity Estimate from Operational Model of Allosterism.
| rmGlu1 WT |
hmGlu1 WT |
rmGlu1 V757L |
hmGlu1 L757V |
|||||
|---|---|---|---|---|---|---|---|---|
| entry | pIC50 (IC50) | est pKB (KB) | pIC50 (IC50) | est pKB (KB) | pIC50 (IC50) | est pKB (KB) | pIC50 (IC50) | est pKB (KB) |
| 1 BAY36-7620 | 6.49 ± 0.03 | 6.62 ± 0.08 | <5 | <5 | <5 | <5 | 6.34 ± 0.03 | 6.18 ± 0.09 |
| (326 nM) | (242 nM) | (>10 μM) | (>10 μM) | (>10 μM) | (>10 μM) | (455 nM) | (667 nM) | |
| 3 DFMTI | 8.08 ± 0.02 | 8.06 ± 0.06 | 7.51 ± 0.09 | 7.75 ± 0.07 | 7.67 ± 0.07 | 7.65 ± 0.09 | 7.86 ± 0.03 | 8.19 ± 0.05 |
| (8 nM) | (9 nM) | (31 nM) | (18 nM) | (21 nM) | (22 nM) | (14 nM) | (7 nM) | |
| 6 VU0410425 | 6.85 ± 0.02 | 6.43 ± 0.04 | <4.5 | 5.17 ± 0.06 | <4.5 | 5.31 ± 0.08 | 6.44 ± 0.08 | 6.45 ± 0.04 |
| (140 nM) | (371 nM) | (>30 μM) | (6.8 μM) | (>30 μM) | (4.8 μM) | (360 nM) | (358 nM) | |
a
Calcium mobilization assay; values are average of n ≥ 3.