Table 5.
Off-target selectivity of lead compounds 19a-c,n,p
| Receptor | 19a | 19b | 19c | 19n | 19p |
|---|---|---|---|---|---|
| ALK1/ACVRL1 | 39.1 | 166.3 | 308.8 | <5 | 89.2 |
| ALK2/ACVR1 | 8.0 | 10.9 | 32.2 | <5 | <5 |
| ALK2 (R206H) | 3.8 | 5.6 | <5 | <5 | |
| ALK3/BMPR1A | <5 | <5 | <5 | <5 | <5 |
| ALK4 | 464 | 568.7 | 596.1 | 192 | 390 |
| ALK5 | 1,260 | 1,267 | 1,285 | 310 | 717 |
| ALK6 | 18.4 | 29.4 | 40.9 | 54.5 | 188 |
| BMPR2 | >10,000 | >50,000 | >50,000 | >50,000 | >50,000 |
| TGFβR2 | 1,250 | 587.2 | 170.7 | 4,590 | 498 |
| AMPK | >10,000 | 13,590 | 18,600 | 20,000 | 11,500 |
| KDR | 5,930 | 13,410 | 20,560 | 9,350 | 36,900 |
| PDGFRβ | 1,250 | 7,450 | >10 000 | 2,820 | 6,903 |
a
Selectivity data were obtained at Reaction Biology (Malvern, PA)