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Fused Pyrazolo Series
| ||||
|---|---|---|---|---|
|
| ||||
| Compd | R | X | Polθ IC50 (μM)a | Microsomal Stability CL (μL/min/mg) |
|
| ||||
| 2 |
|
O | 0.17 | >555 |
| 3 |
|
O | >100 | 16 |
| 4 |
|
O | >100 | 18 |
| 5 |
|
O | >100 | 46 |
| 6 |
|
O | 43 | 23 |
| 7 |
|
O | 0.71 | >555 |
| 8 |
|
O | 10 | 473 |
| 9 |
|
O | 0.24 | >555 |
| 10 |
|
O | 0.95 | >832 |
| 11 |
|
O | 0.52 | >555 |
| 12 |
|
O | 0.56 | >555 |
| 13 |
|
O | 2.3 | >832 |
| 14 |
|
S | 0.017 | >555 |
Picogreen assay: 3nM of Polθ enzyme (n=3)
