Affinity and selectivity values of selected A3AR antagonists
Affinity values are derived from Fredholm et al., 2011, unless otherwise indicated.
| A3AR Antagonists | A1AR Ki | A2AAR Ki | A2BAR Ki | A3AR Ki | A1/A3 | A2A/A3 |
|---|---|---|---|---|---|---|
| nM | ||||||
| MRS1220 | 231a | 25a | N.D. | 0.59a | 391 | 42 |
| MRS1191 | >10,000 (h) | >10,000 (h) | >10,000 (h) | 31.4 (h) | >318 | >318 |
| 40,100 (r) | >10,000 (r) | 1850 (r) | 22 | >5 | ||
| MRS1523 | >10,000 (h) | 3660 (h) | >10,000 (h) | 18.9 (h) | >529 | 194 |
| 15,600 (r) | 2050 (r) | N.D. | 113 (r) | 138 | 18 | |
| N.D. | N.D. | >10,000 (m) | 731 (m) | N.D. | N.D. | |
| VUF-5574 | >10,000 (r) | >10,000 (r) | N.D. | 4.03 (h) | >2481 | >2481 |
| MRE 3008F20 | 1200 (h) | 141 (h) | 2100 (h) | 0.82 (h) | 1463 | 172 |
| MRE 3005F20 | 350 (h) | 100 (h) | 250 (h) | 0.01 (h) | 35,000 | 10,000 |
| OT-7999 | >10,000 (h)a | >10,000 (h)a | N.D. | 0.95 (h)a | >10,526 | >10,526 |
| PSB-10 | 1700 (h) | 2700 (h) | N.D. | 0.44 (h) | 3864 | 6136 |
| PSB-11 | 1640 (h) | 1280 (h) | 2100 (m) | 2.34 (h) | 701 | 547 |
| KF26777 | 1800 (h) | 470 (h) | 620 (h) | 0.20 (h) | 9000 | 2350 |
| Structure A | >10,000 (h)b | 7490 (h)b | N.D. | 4.90 (h)b | 2041 | 1529 |
| 231 (r)b | ||||||