Potency data for probe BI-5121 and control BI-6199
In vitro potency
| Target name | Target information | Species | Assay description | BI-5121 | BI-6199 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| HCRTR1 | Homo sapiens | Eurofins radio-displacement assay (HCRTR1) | IC50 < 3 nM | IC50 = 2.3 µM | ||
| HCRTR2 | Homo sapiens | Eurofins radio-displacement assay (HCRTR2) | IC50 = 140 nM | IC50 > 10 µM |
In cell potency
| Target name | Target information | Species | Assay description | BI-5121 | BI-6199 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| HCRTR1 | Homo sapiens | OX1 ANTA IP1: Activation of the orexin receptors expressed in cell lines results in an increase in intracellular IP3 concentration. IP1, a downstream metabolite of IP3, accumulates in cells following receptor activation and is stable in the presence of LiCl. Using Cisbio™`s HTRF technology with Lumi4TM-Tb cryptate and a suited fluorescence plate reader, this functional response is detectable and quantifiable. | IC50 = 1.6 nM | IC50 = 1.1 µM | ||
| HCRTR2 | Homo sapiens | OX2 ANTA IP2: Activation of the orexin receptors expressed in cell lines results in an increase in intracellular IP3 concentration. IP1, a downstream metabolite of IP3, accumulates in cells following receptor activation and is stable in the presence of LiCl. Using Cisbio™`s HTRF technology with Lumi4TM-Tb cryptate and a suited fluorescence plate reader, this functional response is detectable and quantifiable. | IC50 = 62.6 nM | IC50 = 8.2 µM |