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Chemical starting points identified by screening PKIS2 Screening.
| ||||||||
|---|---|---|---|---|---|---|---|---|
| Cmpd | X | R1 | R2 | R3 | R4 | R5 | GAK Kd (μM) |
Kinase off targetsa |
| 1 | CH | OMe | OMe | OMe | CF3 | H | 31 | 1 |
| 2 | CH | OMe | OMe | OMe | H | 4-pyridyl | (85% at 1 μM) | 18 |
| 3 | N | Br | H | H | OMe | OMe | 29 | 3 |
Number of kinases with over 95% binding at 1 μM in a DiscoverX KINOMEscan® experiment.
