Potency data for probe BAY-091 and control BAY-0361
In vitro potency
| Target name | Target information | Species | Assay description | Compound conc. | BAY-091 | BAY-0361 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| PIP4K2A | Homo sapiens | Quantification of produced ADP with 10 uM ATP: Luminescence readout: ADP-Glo (Promega) | IC50 = 1.3 nM | ||||
| PIP4K2A | Homo sapiens | Quantification of produced ADP with 250 uM ATP: Luminescence readout: ADP-Glo (Promega) | IC50 = 2.6 nM | ||||
| PIP4K2A | Homo sapiens | Quantification of produced PI(4,5)P2 with 10 uM ATP: Homogeneous Time Resolved Fluorescence (HTRF) | IC50 = 8.5 nM | ||||
| PIP4K2A | Homo sapiens | Quantification of produced PI(4,5)P2 with 2 mM ATP: Homogeneous Time Resolved Fluorescence (HTRF) | IC50 = 16.4 nM | ||||
| PIP4K2A | Homo sapiens | Eurofins Kinase panel (PIP4K2A) | 1 µM | IC50 = 21 nM | IC50 = 271 nM |
In cell potency
| Target name | Target information | Species | Assay description | BAY-091 | BAY-0361 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| cell lysate | None | CETSA lysates: Cellular thermal shift assay at 60 °C to test cellular engagement | EC50 = 1.8 µM ± 0.400 µM | |||
| intact cells | None | CETSA intact cells: Cellular thermal shift assay at 56 °C to test cellular engagement | EC50 = 1.1 µM ± 0.200 µM |