TABLE 1.
Selectivity of Ex26 on S1P receptors
Ex26 displays excellent selectivity for S1P1 over other S1P receptors. It also does not exhibit any detectable agonist activity on any S1P receptor.
| Receptor | Antagonist IC50 | Agonist EC50 |
|---|---|---|
| nM | nM | |
| S1P1 | 0.93 | >10,000 |
| S1P2 | >10,000 | >10,000 |
| S1P3 | >10,000 | >10,000 |
| S1P4 | 4900 | >10,000 |
| S1P5 | 3100 | >10,000 |
Ex26, 1-(5′-((1-(4-chloro-3-methylphenyl)ethyl)amino)-2'-fluoro-3,5-dimethyl-[1,1'-biphenyl]-4-ylcarboxamido)cyclopropanecarboxylic acid; S1P, sphingosine 1-phosphate.