Potency data for probe BAY-069 and control BAY-771
In vitro potency
| Target name | Target information | Species | Assay description | BAY-069 | BAY-771 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BCAT1 | Homo sapiens | Biochemical assay (BCAT1) | IC50 = 27 nM | IC50 = 6.5 µM | ||
| BCAT2 | Homo sapiens | Biochemical assay (BCAT2) | IC50 = 130 nM | IC50 = 10.8 µM | ||
| GOT1 | Homo sapiens | Aspartate transaminase assay (GOT1) | IC50 > 50 µM | |||
| GOT2 | Homo sapiens | Aspartate transaminase assay (GOT2) | IC50 > 50 µM |
In cell potency
| Target name | Target information | Species | Assay description | BAY-069 | BAY-771 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BCAT1 | U-87-MG (high BCAT1 expressing) cells | Homo sapiens | Cellular mechanistic assay – BCAA measurement (U-87-MG cells) | IC50 = 358 nM | IC50 = 6.2 µM | |
| BCAT2 | MDA-MB-231 (high BCAT2 expressing) cells | Homo sapiens | Cellular mechanistic assay – BCAA measurement (MDA-MB-231 cells) | IC50 = 874 nM |