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Kinase selectivity of current clinical FAK inhibitors.
| Compound | IC50 values for in vitro kinase inhibition [nM] (assay type) | # kinases with IC50 < 1 μM | Reference | |
|---|---|---|---|---|
| FAK | PYK2 | |||
| IN10018 (BI 853520) | 1 (DELFIA) 38.1 (Z-LYTE™) |
>50,000 (DELFIA) 2000 (Z-LYTE™) |
4 | 48 |
| Defactinib (VS-6063) (PF-04554878) | 0.47 (Kinobeads) 0.6 (Kinase assay) |
423 (Kinobeads) 0.6 (Kinase assay) |
9 | 32,49 |
