Table 2.
The inhibition kinetics of PAEs to UGTs, including IC50, inhibition kinetic type and parameters.
| PAEs-UGTs | IC50(μM) | inhibition type | Ki (μM) |
|---|---|---|---|
| BBOP-UGT1A6 | 35.1 | noncompetitive | 15.5 |
| BBZP-UGT1A6 | 53.2 | noncompetitive | 52.3 |
| BBOP-UGT1A7 | 18.2 | competitive | 23.6 |
| BBZP-UGT1A7 | 19.5 | competitive | 12.2 |
| DiPP-UGT1A9 | 14.7 | competitive | 5.61 |
| DiBP-UGT1A9 | 7.03 | competitive | 2.79 |
| DCHP-UGT1A9 | 1.46 | competitive | 1.07 |
| DBP-UGT1A9 | 17.6 | competitive | 22.8 |
| BBZP-UGT1A9 | 5.54 | competitive | 0.84 |
| BBOP-UGT1A9 | 28.3 | noncompetitive | 73.7 |
| DMEP-UGT1A9 | 18.2 | competitive | 4.51 |
| DPP-UGT1A9 | 18.5 | competitive | 1.74 |
| DHP-UGT1A9 | 25.4 | competitive | 0.58 |
| DiBP-UGT2B4 | 5.89 | noncompetitive | 6.79 |
| DBP-UGT2B4 | 11.9 | noncompetitive | 4.93 |
| DAP-UGT2B4 | 14.3 | competitive | 6.73 |
| BBZP-UGT2B4 | 13.8 | noncompetitive | 7.23 |