Selectivity comparison between PF-4800567 and PF-670462 Data shown are the percentage of inhibition at the indicated concentration of each inhibitor.
PF-4800567 | PF-670462 | |||||
|---|---|---|---|---|---|---|
| 1 μM | 10 μM | 1 μM | 10 μM | |||
| CK1γ2 | 1 | N.D. | 2 | N.D. | ||
| GSK3β | N.D. | 0 | N.D. | 57 | ||
| p38 cascade | 2 | 3 | 100 | 100 | ||
| MLCK | N.D. | 4 | N.D. | 53 | ||
| PRKC B2 | 2 | 7 | 29 | 75 | ||
| PKACα | 1 | 23 | 78 | 98 | ||
| EphA2 | 16 | 39 | 20 | 68 | ||
| SRC | 9.5 | 47 | N.D. | 58 | ||
| VEGFR2 | 11 | 51 | 20 | 70 | ||
| LCK | 32 | 57 | 55 | 88 | ||
| HGK | 20 | 75 | 97 | 99 | ||
| EGFR | 69 | 83 | 76 | 99 | ||
CK1γ2, casein kinase 1γ2; GSK3β, glycogen synthase kinase 3β; p38 cascade, p38α coupled to MAPKAPK2; MLCK, myosin light-chain kinase; PRKC B2, protein kinase C B2; PKAC α, protein kinase A catalytic subunit α; VEGFR2, vascular endothelial growth factor receptor 2 tyrosine kinase; EGFR, epidermal growth factor receptor tyrosine kinase; N.D., not determined; LCK, lymphocyte-specific protein tyrosine kinase; HGK, HPK/GCK-line kinase