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| IC50 (μM) |
|||||
|---|---|---|---|---|---|
| compd | PLD1a | PLD2a | Calu-1b | MDR1 ERc | cLogP/MPOd |
| 17 | 0.13 | >10 | 0.18 | 24 | 2.3/5.8 |
| 18 | 0.12 | >10 | 0.98 | 17 | 1.6/5.8 |
| 19 | 0.043 | >10 | 0.058 | 8.6 | 1.8/5.8 |
Biochemical inhibition of PLD1/2 was determined by immunoprecipitation on a plate (IPoP) of PLD1/2 from HEK cells.
Cellular assay performed with Calu-1 cell line.
Rat or human liver microsomes.
Efflux ratio determined by measuring Papp(B-A)/Papp(A-B) in MDR1-MDCK.
