PXR transactivation results for 30 compounds tested in human and cynomolgus monkey PXR transactivation assays
| Substancea | PXR Transactivation (Human/Cynomolgus) | ||
|---|---|---|---|
| Emax | EC50 | IIAb | |
| %RIF | μM | Emax/EC50 | |
| Hyperforinc | 148/155 | 0.04/0.08 | 3610/2067 |
| SR-12813 | 120/163 | 0.16/0.63 | 736/259 |
| Clotrimazole | 115/94 | 1.4/1.0 | 82/94 |
| Rosiglitazone | 109/94 | ∼25/∼25 | 4.4/3.8 |
| 1,9-Dideoxy-forskolin | 103/109 | 1.4/7.5 | 74/15 |
| Reserpine | 103/16 | 2.7/50 | 38/0.3 |
| Rifampicin | 101/137 | 0.84/5.1 | 121/27 |
| Glimepiride | 98/96 | 7.5/19 | 13/5.1 |
| Ritonavir | 97/112 | 1.7/4.5 | 57/25 |
| Pioglitazone | 92/69 | ∼25/∼25 | 3.7/2.8 |
| CITCO | 87/109 | 1.9/4.3 | 46/25 |
| Sulfinpyrazone | 73/11 | ∼25/>50 | 2.9/0.2 |
| Verapamil | 71/180 | 3.5/3.6 | 20/50 |
| Nifedipine | 70/69 | 1.7/4.5 | 41/15 |
| Artemisinin | 67/79 | 29/14 | 2.3/5.8 |
| Terbinafine | 63/40 | 4.8/5.0 | 13/8.0 |
| Paclitaxel | 60/40 | 0.55/2.2 | 109/18 |
| Troleandomycin | 60/116 | 4.1/10 | 15/12 |
| Troglitazone | 55/65 | 4.1/4.1 | 13/16 |
| Mifepristone | 53/49 | 1.8/1.6 | 29/31 |
| PCN | 50/113 | ∼25/∼25 | 2.0/4.5 |
| Celecoxib | 36/94 | 2.5/8.3 | 14/11 |
| Phenytoin | 33/23 | 28/16 | 1.2/1.4 |
| Meclizine | 25/29 | 8.3/6.2 | 3.0/4.7 |
| TCPOBOP | 22/44 | 4.3/5.9 | 5.1/7.5 |
| Carbamazepine | 21/21 | >50/>50 | 0.4/0.4 |
| Probenecid | 9/7 | >50/>50 | 0.2/0.1 |
| Phenobarbital | 3/1 | >50/>50 | 0.1/0.0 |
| Dexamethasone | 0/4 | >50/>50 | 0.0/0.1 |
| Methotrexate | 0/2 | >50/>50 | 0.0/0.0 |