Table 1.
Affinities of FR and YM derivatives and analogs determined in competition-binding assays versus [³H]PSB-15900 compared to published potencies determined in functional assays
| Affinities (pKi ± SD) | Published potencies (pIC50) | |
|---|---|---|
| FR900359 | 9.23 ± 0.29 | 7.49c |
| FR-1 | 8.80 ± 0.23 | n.a. |
| FR-2 | 9.02 ± 0.22 | 7.79 |
| FR-3/4 | 8.23 ± 0.33 | n.a. |
| FR-6 | 7.26 ± 0.38 | 5.56d |
| [³H]PSB-15900 | 8.19 ± 0.16a | n.a. |
| YM-254890 | 8.23 ± 0.48 | 7.02c |
| YM-1 | 6.27 ± 0.03 | 6.06c |
| YM-3 | 5.57 ± 0.02 | 4.99c |
| YM-7 | 6.45 ± 0.38 | 6.00c |
| YM-8 | 6.43 ± 0.35 | 5.63c |
| YM-9 | 5.77 ± 0.24 | 5.01c |
| YM-10 | 7.68 ± 0.20 | 6.74c |
| YM-11 | 6.62 ± 0.48 | 6.38e |
| YM-12 | 7.15 ± 0.31 | 6.35e |
| YM-13 | 7.23 ± 0.33 | 6.57e |
| YM-14 | 7.54 ± 0.36 | 6.72e |
| YM-15 | 7.02 ± 0.20 | 6.01e |
| YM-18 | 7.88 ± 0.22 | 6.52e |
| [³H]PSB-16254 | 7.80b | – |
Affinity ata is expressed as mean ± SD from 3 to 6 independent experiments, performed in duplicate. n.a., no published data available.
a
pKD value determined by saturation binding.
b
pKD value determined by saturation binding.32
c
determined by IP1 accumulation assays.22
d
determined by dynamic mass redistribution.19
e
determined by IP1 accumulation assays.20