Potency for inhibition of glutamate-evoked responses in calcium flux assays
Data are represented as the mean pIC50 ± standard deviation of multiple measurements. The numbers in parentheses indicate the number of measurements performed. Unless otherwise stated, all constructs are human.
| GYKI-53655 | CP-465022 | JNJ-55511118 | JNJ-56022486 | |
|---|---|---|---|---|
| GluA1o-γ8 | 5.65 ± 0.46 (14) | 6.57 ± 0.24 (20) | 8.33 ± 0.28 (22) | 8.02 ± 0.35 (10) |
| GluA1o+ γ8 | 5.72 ± 0.42 (2) | 6.26 ± 0.25 (7) | 7.95 ± 0.21 (7) | 7.79 ± 0.22 (6) |
| rat(GluA1o- γ8) | 5.00 ± 0.41 (2) | 6.18 ± 0.37 (7) | 7.89 ± 0.3 (7) | 7.45 ± 0.41 (5) |
| mouse(GluA1o- γ8) | 5.19 ± 0.24 (2) | 6.03 ± 0.23 (8) | 7.87 ± 0.31 (7) | 7.53 ± 0.44 (5) |
| monkey(GluA1o+ γ8) | 5.81 ± 0.66 (2) | 6.28 ± 0.25 (4) | 7.88 ± 0.15 (7) | 7.65 ± 0.21 (6) |
| dog(GluA1o+γ8) | 5.63 ± 0.38 (2) | 6.16 ± 0.16 (4) | 7.82 ± 0.28 (7) | 7.53 ± 0.27 (6) |
| GluA1i+γ8 | 5.39 ± 0.46 (2) | 6.02 ± 0.17 (8) | 7.91 ± 0.39 (7) | 7.58 ± 0.33 (5) |
| GluA2i+γ8 | 5.25 ±–(1) | 6.06 ± 0.22 (6) | 8.13 ± 0.35 (2) | 7.5 ± 0.11 (2) |
| GluA3o+γ8 | 5.24 ± 0.09 (2) | 6.15 ± 0.3 (9) | 7.42 ± 0.38 (6) | 7.03 ± 0.1 (4) |
| GluA4o+γ8 | 5.8 ± 0 (2) | 6.28 ± 0.46 (2) | 7.8 ± 0.26 (4) | 7.49 ± 0.11 (4) |
| GluA1o+γ8+CNIH2 | 5.54 ± 0.5 (2) | 6.18 ± 0.52 (12) | 7.87 ± 0.31 (7) | 7.66 ± 0.28 (4) |
| GluA1i | 5.11 ± 0.29 (2) | 5.94 ± 0.15 (4) | >5 (6) | >5 (4) |
| GluA1o+CNIH2 | 4.96 ± 0.12 (2) | 5.93 ± 0.27 (7) | >5 (6) | >5 (4) |
| GluA1o+γ2 | 6.03 ± 0.11 (2) | 6.55 ± 0.38 (5) | >5 (5) | >5 (4) |
| GluA1o+γ3 | 6.18 ± 0.3 (2) | 6.72 ± 0.23 (8) | >5 (6) | >5 (4) |
| GluA1o+γ4 | 5.85 ± 0.35 (2) | 6.45 ± 0.46 (8) | >5 (6) | >5 (4) |
| GluA1o+γ7 | 5.84 ± 0.19 (2) | 6.55 ± 0.34 (5) | >5 (6) | >5 (3) |