TABLE 2.
FPR1 |
FPR2 |
|||||
---|---|---|---|---|---|---|
Compound No. |
Binding Ki |
Agonist EC50 |
Antagonist IC50 |
Binding Ki |
Agonist EC50 |
Antagonist IC50 |
nM | ||||||
Pyrrolidine bis-diketopiperazine scaffold | ||||||
a: 1754-113 | 3 | a | 1,070 | b | a | c |
b: 1754-56 | 2 | a | 139 | 1,320 | 1,300 | NA |
c: 1754-26 | 46 | a | 2,680 | 70 | a | 3,480 |
d: 1754-20 | b | a | c | 15 | a | 452 |
e: 1754-19 | 3,370 | a | c | 6 | a | 1,410 |
f: 1754-31 | b | a | c | 1 | a | 81 |
g: 1754-49 | 2,320 | a | c | 33 | 144 | NA |
Polyphenylurea scaffold | ||||||
h: 1753-103 | 4 | 131 | NA | b | a | c |
NA, not applicable.
No agonistic activity at up to 12 µM.
Ki greater than 10,000 nM.
No antagonistic activity at up to 10 µM.