Potency data for probe PF-04418948 and control PF-04475866
In vitro potency
| Target name | Target information | Species | Assay description | PF-04418948 | PF-04475866 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PTGER2 | Homo sapiens | Inhibition of binding to PTGER2 | IC50 = 5 nM | IC50 = 1.3 µM | ||
| PTGFR | Homo sapiens | Binding assay (PTGFR) | Ki > 10 µM (n=2) | PMID: 21595651 | ||
| PTGIR | Homo sapiens | Binding assay (PTGIR) | Ki > 10 µM (n=2) | PMID: 21595651 | ||
| TBXA2R | Homo sapiens | Binding assay (TBXA2R) | Ki > 10 µM (n=2) | PMID: 21595651 | ||
| LTB4R | Homo sapiens | Binding assay (LTB4R ) | Ki = 4.8 µM | PMID: 21595651 |
In cell potency
| Target name | Target information | Species | Assay description | PF-04418948 | PF-04475866 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PTGER2 | Homo sapiens | Functional native assay with human myometrium: Parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent K(B) of 5.4 nM | KB = 5.4 nM (n=4) | PMID: 21595651 | ||
| PTGER2 | Homo sapiens | Functional reporter assay | KB = 1.8 nM (n=4) | PMID: 21595651 |