Potency data for probe PF-04457845 and control PF-04875474
In vitro potency
| Target name | Target information | Species | Assay description | PF-04457845 | PF-04875474 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| FAAH | Homo sapiens | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 1 min) | IC50 = 50.4 nM ± 5.500 nM (n=3) | PMID: 21505060 | ||
| FAAH | Homo sapiens | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 15 min) | IC50 = 32.4 nM ± 0.990 nM (n=3) | PMID: 21505060 | ||
| FAAH | Homo sapiens | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 30 min) | IC50 = 10.7 nM ± 1.000 nM (n=3) | PMID: 21505060 | ||
| FAAH | Homo sapiens | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min) | IC50 = 7.4 nM ± 0.630 nM | PMID: 21505060 | ||
| FAAH | Homo sapiens | Binding assay | IC50 > 100 µM | PMID: 21505060 |
In cell potency
| Target name | Target information | Species | Assay description | PF-04457845 | PF-04875474 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| FAAH | human membrane proteasomes | Homo sapiens | Proteaseome | IC50 = complete inhibition% | PMID: 21505060 |