Potency data for probe BAY-277 and control BAY-8805
In vitro potency
| Target name | Target information | Species | Assay description | BAY-277 | BAY-8805 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| METAP2 | Homo sapiens | METAP2 biochemical assay (human) | IC50 = 5.8 nM | IC50 = 5.7 nM | ||
| METAP2 | Mus musculus | METAP2 biochemical assay (mouse) | IC50 = 5.9 nM |
In cell potency
| Target name | Target information | Species | Assay description | BAY-277 | BAY-8805 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| METAP2 | HT1080 cells | Homo sapiens | Degradation in HT1080 cells (CE): Capillary electrophoresis (CE) | DC50 = 8.93 nM | DC50 > 1 µM | |
| METAP2 | HT1080 cells | Homo sapiens | Degradation in HT1080 cells (CE) Dmax: Capillary electrophoresis (CE) | Dmax = 88.5% | ||
| METAP2 | HUVEC cells | Homo sapiens | Degradation in HUVEC cells (WB): Western Blot (WB) | DC50 = 0.2 nM | DC50 > 100 nM | |
| METAP2 | HUVEC cells | Homo sapiens | Degradation in HUVEC cells (WB) Dmax: Western Blot (WB) | DCmax = 94% | ||
| METAP2 | HUVEC cells | Homo sapiens | 2D HUVEC cells proliferation assay | IC50 = 12 nM | IC50 = 450 nM |