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Displacement of the Antagonist Radioligand [3H]CPX and the Degree of Shift of the Displacement Curve in the Presence of 1 mM GTP
| compd |
Ki value (μM) or % displacement at 10−4 Ma
|
GTP Shiftb | |
|---|---|---|---|
| A1 (−GTP) | A1 (+GTP) | ||
| 10a | 40 | nd | |
| 12c | 35 | nd | |
| 18 | 36 | nd | |
| 21 | 13 | 30 | 2.3 |
| 22 | 8.4 | 12 | 1.4 |
| 23 | 1.7 | 8.3 | 4.9 |
| 25 | 12 | 21 | 1.7 |
| 26 | 31 | nd | |
| 27 | 37 | nd | |
| 28b | 12 | nd | |
Average of two determinations.
nd = not determined.
Ratio of Ki values in the presence and absence of GTP.
