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Table 5 Summary of inhibition of CYP450 by (r)-SJ733 and (r)-SJ311

From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

CYP (r)-SJ733 (r)-SJ311 Probe substrate Probe substrate metabolite
CYP1A2 − 5, 10.8%a 5, 0.5% Ethoxy-resorufin Resorufin
CYP2C9 34, 17% 19, 15% Diclofenac 4′-Hydroxy diclofenac
CYP2C19 5, 5% 12, − 2% S-mephenytoin 4′-Hydroxy mephenytoin
CYP2D6 7, 9% 11, − 4% Bufuralol 1′-Hydroxy bufuralol
CYP3A4 42, 33% 54, 52% Midazolam 1′-Hydroxy midazolam
  1. aValues in columns represent replicate measurements. Compounds were tested at 10 µM
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