Table 1.
Summary of selected DIVERSet ATPase activators.
| Skeletal SR | Cardiac SR | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Compound | ATPase Activity | Ca2+ Uptake Activity | ATPase Activity | Ca2+ Uptake Activity | |||||
| N, Cluster | DIVERSet ID | Percent Increase | EC50 | Percent Increase | EC50 | Percent Increase | EC50 | Percent Increase | EC50 |
| 1, 1 | 67200668 | 50 ± 25 | 40 ± 21 | 27 ± 3 | 28 ± 9 | 42 ± 12 | 31 ± 10 | 32 ± 2 | 37 ± 4 |
| 2, 1 | 75082844 | 36 ± 2 | 4.0 ± 0.5 | 15 ± 1 | 2.2 ± 0.4 | 33 ± 3 | 2.9 ± 0.6 | 12 ± 1 | 1.2 ± 0.2 |
| 3, 1 | 76145530 | 54 ± 2 | 7.3 ± 0.5 | 20 ± 1 | 3.4 ± 0.5 | 48 ± 4 | 6.7 ± 1.0 | 37 ± 3 | 3.5 ± 0.7 |
| 4, 1 | 81260867 | 53 ± 2 | 5.4 ± 0.4 | 14 ± 2 | 1.4 ± 0.5 | 58 ± 4 | 4.8 ± 0.6 | 24 ± 1 | 1.6 ± 0.3 |
| 5, 1 | 11966966 | 41 ± 3 | 9.0 ± 1.0 | 10 ± 1 | 1.4 ± 0.6 | 58 ± 6 | 7.7 ± 2 | 16 ± 3 | 1.0 ± 0.7 |
| 6, 1 | 25365366 | 45 ± 8 | 24 ± 6 | 9 ± 1 | 4 ± 1 | 63 ± 17 | 29 ± 12 | 17 ± 1 | 3.8 ± 0.6 |
| 7, 2 | 31221514 | 41 ± 3 | 3.6 ± 0.4 | 14 ± 2 | 1.4 ± 0.4 | 51 ± 3 | 2.9 ± 0.3 | 24 ± 3 | 1.3 ± 0.4 |
| 8, 2 | 39746187 | 45 ± 2 | 4.0 ± 0.4 | 13 ± 1 | 1.3 ± 0.4 | 43 ± 2 | 3.4 ± 0.3 | 18 ± 2 | 0.8 ± 0.3 |
| 9, 2 | 84875791 | 72 ± 2 | 13.3 ± 0.7 | 31 ± 7 | 8 ± 5 | 85 ± 5 | 11 ± 1 | 33 ± 3 | 4.0 ± 0.8 |
| 10, 3 | 19784159 | 57 ± 3 | 10 ± 1 | 11 ± 3 | 4 ± 2 | 55 ± 2 | 7.5 ± 0.4 | 16 ± 3 | 1.6 ± 0.7 |
| 11, 3 | 27035959 | 61 ± 2 | 7.2 ± 0.4 | 9.1 ± 0.8 | 1.2 ± 0.3 | 62 ± 2 | 6.4 ± 0.4 | 18 ± 2 | 1.2 ± 0.4 |
| 12, 3 | 60405307 | 41 ± 2 | 3.4 ± 0.4 | 6.5 ± 0.5 | 0.6 ± 0.2 | 29 ± 1 | 2.3 ± 0.3 | −10 ± 3 | 1.3 ± 0.1 |
| 13, 4 | 71721828 | 36 ± 4 | 3.2 ± 0.6 | 8 ± 2 | 1.1 ± 0.6 | 36 ± 4 | 2.9 ± 0.6 | 21 ± 10 | 1.8 ± 2 |
| 14, 4 | 32014423 | 25 ± 3 | 3.3 ± 0.6 | 8 ± 2 | 1.1 ± 0.6 | 56 ± 3 | 5.2 ± 0.5 | 28 ± 5 | 2.5 ± 0.9 |
| 15, 5 | 19396790 | 30 ± 1 | 30 ± 12 | -- | -- | 46 ± 6 | 16 ± 3 | 6 ± 5 | 5 ± 11 |
| 16, 5 | 33804556 | 25 ± 1 | 3.0 ± 0.3 | −10 ± 2 | 7 ± 13 | 26 ± 2 | 2.2 ± 0.4 | −27 ± 3 | 8.9 ± 2 |
| 17, 5 | 39779602 | 42 ± 4 | 16 ± 3 | -- | -- | 62 ± 5 | 9.4 ± 1 | -- | -- |
| 18, 6 | 81801810 | 39 ± 1 | 5.2 ± 0.3 | 8.9 ± 0.1 | 1.1 ± 0.3 | 37 ± 1 | 4.3 ± 0.3 | 12 ± 1 | 0.9 ± 0.2 |
| 19, 7 | 30616130 | 42 ± 2 | 7.3 ± 0.8 | 7.2 ± 0.1 | 1.8 ± 0.7 | 22 ± 2 | 6.3 ± 0.4 | 8 ± 1 | 2.4 ± 0.6 |
Compounds are listed 1–19, along with corresponding physicochemical cluster number (see Supporting Information, Table S1) and DIVERSet ID #, along with mean ± SD of percent increase and EC50 of a compound for ATPase and Ca2+ uptake activities for both skeletal and cardiac SR preparations (n = 3). Dashed entries indicate no observable effect. All CRCs for data in this table are included in Supporting Information (Figure S1).