Table 2.
FP receptor antagonist and purported antagonist, affinity and/or functional potencies from various assay systems
| Compound | Antagonist receptor binding affinity or functional potency parameters at prostanoid receptors (IC50 or Ki or Kb, nM) | |||||||
|---|---|---|---|---|---|---|---|---|
| DP | EP1 | EP2 | EP3 | EP4 | FP | IP | TP | |
| AL‐8810 | >30 000 | nd | >30 000 | nd | >30 000 | 285–426 (competitive) | >100 000 | >100 000 |
| AL‐3138 | >100 000 | nd | >100 000 | nd | >100 000 | 86;182–296 (non‐competitive) | >10 000 | nd |
| AS604872 | >10 000 | >10 000 | 650 | >10 000 | >10 000 | 35–323 (undefined) | >10 000 | >10 000 |
| AGN‐211377 | 49 ± 16 | 266 ± 67 | nd | 5008 ± 2571 | 117 ± 29 | 61 ± 16 (apparently non‐competitive) | nd | 11 ± 6 |
| Phloretin | ~4250 | nd | ~4229 | nd | nd | 1400–5248 (non‐competitive) | 2119 | 3383 |
| THG‐113.31 (PDC31) | – | – | – | – | – | ~30 (non‐competitive) | – | – |