TABLE 2.
Structure-activity relationships for Y2R-selective antagonists SF numbers of compounds from HTS are in boldface type.
| ID | R | IC50(Maximum
Inhibition) |
CC50(Maximum Toxicity) | ID | R1 | R2 | IC50(Maximum
Inhibition) |
CC50(Maximum Toxicity) | ||
|---|---|---|---|---|---|---|---|---|---|---|
| Y2R | Y1R | Y2R | Y1R | |||||||
|
|
|||||||||
| μM | μM | μM | μM | |||||||
| SF-11 |
|
0.199 ± 0.01 | >35.4 (inactive) | >33 | SF-21 | Cl |
|
0.44 ± 0.03 | >35.4 (10 ± 2%) | 19.7 ± 7.2 |
| SF-12 |
|
1.1 ± 0.1 | >35.4 (5 ± 4%) | >99 (37 ± 8%) | SF-22 | CH3 |
|
0.75 ± 0.03 | >35.4 (inactive) | 61 ± 30 |
| SF-13 |
|
1.3 ± 0.1 | >35.4 (inactive) | >33 | SF-23 | CH3 |
|
2.1 ± 0.2 | >35.4 (inactive) | >33 |
| SF-14 |
|
2.99 ± 0.1 | >35.4 (inactive) | >99 (49 ± 6%) | SF-24 | Cl |
|
3.96 ± 0.3 | >35.4 (inactive) | >33 |
| SF-15 |
|
4.9 ± 0.57 | >35.4 (4 ± 3%) | >99 (41 ± 6%) |
|
|||||
| SF-16 |
|
>35.4 (43 ± 5%) | >35.4 (inactive) | >33 | SF-31 |
|
1.2 ± 0.1 | >35.4 (inactive) | >99 (43 ± 7%) | |
|
SF-32 |
|
4.9 ± 0.1 | >35.4 (inactive) | >99 (27 ± 11%) | |||||
| SF-41 |
|
4.4 ± 0.04 | >35.4 (inactive) | >99 (35 ± 9%) | SF-33 |
|
5.5 ± 0.8 | >35.4 (34 ± 4%) | 30.8 ± 2.7 | |
| SF-42 |
|
8.6 ± 0.5 | >35.4 (inactive) | >99 (9 ± 8%) | SF-34 |
|
17.3 ± 6.7 | 17.3 ± 3.4 | >33 | |
| SF-35 |
|
>11.8 | >11.8 | 17.2 ± 0.4 | ||||||
| SF-36 |
|
>35.4 (46 ± 4%) | >35.4 (36 ± 11%) | >11 | ||||||
| SF-37 |
|
>35.4 (45 ± 7%) | >35.4 (inactive) | >33 | ||||||
| SF-38 |
|
>35.4 (43 ± 4%) | >35.4 (6 ± 3%) | >33 | ||||||
| SF-39 |
|
>35.4 (4 ± 2%) | >35.4 (inactive) | 22.9 ± 2.5 | ||||||