Potency data for probe BAY 1753011 and control BAY-2297
In vitro potency
| Target name | Target information | Species | Assay description | BAY 1753011 | BAY-2297 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| AVPR1A | recombinant; full length | Homo sapiens | Radiometric AVPR1A binding assay (Eurofins #287530) | Ki = 0.5 nM | Ki > 10 µM | Eurofins assay |
| AVPR2 | recombinant; full length | Homo sapiens | Radiometric AVPR2 binding assay (Eurofins #287610) | Ki = 0.6 nM | Ki > 10 µM | Eurofins assay |
| AVPR1B | recombinant; full length | Homo sapiens | Radiometric AVPR1B binding assay (Eurofins #287560) | Ki > 10 µM | Ki > 10 µM | Eurofins assay |
| OXTR | recombinant; full length | Homo sapiens | Radiometric OXTR binding assay (Eurofins #260900) | Ki = 5.1 nM | Ki > 10 µM | Eurofins assay |
In cell potency
| Target name | Target information | Species | Assay description | BAY 1753011 | BAY-2297 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| AVPR1A | recombinant CHO K1 cell line; full length | Homo sapiens | Assay with bioluminescence detection (AVPR1A): The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. | IC50 = 3.6 nM | IC50 > 10 µM | PMID: 31274842 |
| AVPR2 | recombinant CHO K1 cell line; full length | Homo sapiens | Assay with bioluminescence detection (AVPR2): The vasopressin receptor cells react to stimulation of the recombinantly expressed V2a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. | IC50 = 1.7 nM | IC50 > 10 µM | PMID: 31274842 |