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Primary screening of compounds 4a–m on DYRK1A and DYRK1B
| Entry |
| % inhibitiona,b at 1 μM | IC50 for DYRK1Aa,b in nM |
|---|
| 1 | 4a | R5 = H | R′′ = 10-OMe | DYRK1A <5% | nd |
| DYRK1B <5% |
| 2 | 4b | R5 = H | R′′ = 9-OMe | DYRK1A <5% | nd |
| DYRK1B <5% |
| 3 | 4c | R5 = H | R′′ = 8-OMe | DYRK1A <5% | nd |
| DYRK1B <5% |
| 4 | 4d | R5 = H | R′′ = 7-OMe | DYRK1A 23% | nd |
| DYRK1B 7% |
| 5 | 4e | R5 = OMe | R′′ = H | DYRK1A 91% | 52 |
| DYRK1B 68% |
| 6 | 4f | R5 = OMe | R′′ = 10-OMe | DYRK1A 28% | nd |
| DYRK1B <5% |
| 7 | 4g | R5 = OMe | R′′ = 9-OMe | DYRK1A 25% | nd |
| DYRK1B <5% |
| 8 | 4h | R5 = OMe | R′′ = 8-OMe | DYRK1A <5% | nd |
| DYRK1B <5% |
| 9 | 4i | R5 = OH | R′′ = H | DYRK1A 98% | 105 |
| DYRK1B 89% |
| 10 | 4j | R5 = OH | R′′ = 9-OMe | DYRK1A 99% | 116 |
| DYRK 1B 93% |
| 11 | 4k | R5 = OH | R′′ = 8-OMe | DYRK1A 97% | 35 |
| DYRK1B 78% |
| 12 | 4l | R5 = OH | R′′ = 7-OMe | DYRK1A 93% | 54 |
| DYRK1B 78% |
| 13 | 4m | R5 = F | R′′ = 8-OMe | DYRK1A <5% | nd |
| DYRK1B <5% |