IC50 values of transition-state analogs for wild-type and mutant UGT1*6
| Inhibitor | IC50 | ||
|---|---|---|---|
| UGT1*6 | H54A | R52A | |
| μM | |||
| 7,7,7-Triphenylheptanoic acid | 46 | 31 | 46 |
| PP 37 | 332 | 314 | 267 |
| PP 50A | 82 | 123 | N.D. |
| PP 50B | 127 | 145 | 80 |
| PP 55A | 260 | 230 | 314 |
| PP 55B | 168 | 213 | 170 |
PP 37, 5′-O-[[(2-decanoylamino-3-hydroxy-3-phenyl-propyloxycarbonyl)amino]sulfonyl]uridine; PP 50A and 50B, l- and d-, 5′-O[[(2-decanoylamino-3-phenyl-propyloxycarbonyl)amino]sulfonyl]-2′,3′-O-isopropylideneuridine; PP 55A and 55B, l- andd-5′-O-[[(2-decanoylamino-3-phenyl-propyloxycarbonyl)amino]sulfonyl]uridine. N.D., not determined.