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In vitro potency and selectivity of BR103354.
| MW | clogP | IC50 (nM)a | SI indexb (PREP/FAP) | ||||
|---|---|---|---|---|---|---|---|
| FAP | PREP | DPP4 | DPP2 | DPP9 | |||
| 415.42 | 1.907 | 14 | 387 | > 100,000 | n.d | 5,036 | 27.6 |
aThe inhibitory potency of BR103354 on FAP and selectivity against DPP family enzymes were determined by fluorometric assay using AMC substrates and presented as IC50 values. bSI means selectivity index (calculated as [IC50(PREP)/IC50(FAP)]); n.d., not detected.
