Potency data for probe BAY-439 and control BAY-163
In vitro potency
| Target name | Target information | Species | Assay description | BAY-439 | BAY-163 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PLA2G5 | recombinant human protein | Homo sapiens | Biochemical human PLA2G5 assay: Substrate: Red/Green BODIPY® PC-A2; PLA2-G5-dependent increase in BODIPY® FL fluorescence emission was measured in a Pherastar plate reader (BMG) at excitation and dual emission wavelengths of 485 nm and 530/590 nm, respectively. | IC50 = 7 nM | IC50 > 25 µM | Slide 10 in BAY-439 Inhibitor for PLA2G5.pdf |
| PLA2G5 | recombinant mouse protein | Mus musculus | Biochemical mouse PLA2G5 assay: Substrate: Red/Green BODIPY® PC-A2; PLA2-G5-dependent increase in BODIPY® FL fluorescence emission was measured in a Pherastar plate reader (BMG) at excitation and dual emission wavelengths of 485 nm and 530/590 nm, respectively. | IC50 = 8 nM | IC50 > 20 µM | Slide 10 in BAY-439 Inhibitor for PLA2G5.pdf |
| PLA2G5 | recombinant rat protein | Rattus norvegicus | Biochemical rat PLA2G5 assay: Substrate: Red/Green BODIPY® PC-A2; PLA2-G5-dependent increase in BODIPY® FL fluorescence emission was measured in a Pherastar plate reader (BMG) at excitation and dual emission wavelengths of 485 nm and 530/590 nm, respectively. | IC50 = 18 nM | IC50 > 20 µM | Slide 10 in BAY-439 Inhibitor for PLA2G5.pdf |
| PLA2G5 | Homo sapiens | SPR (PLA2G5): in presence of 10mM Ca2+, pH 4.5 | KD = 214 nM | KD > 10 µM | ||
| PLA2G4A | recombinant human protein | Homo sapiens | Biochemical human PLA2G4A assay | IC50 > 40 µM | ||
| PLA2G7 | recombinant human protein | Homo sapiens | Biochemical human PLA2G7 assay | IC50 > 40 µM | IC50 > 20 µM | |
| PLA2G2A | recombinant human protein | Homo sapiens | Biochemical human PLA2G2A assay | IC50 = 788 nM | IC50 > 20 µM | |
| PLA2G10 | recombinant human protein | Homo sapiens | Biochemical human PLA2G10 assay | IC50 = 2.85 µM | IC50 = 14.3 µM | |
| PLCB3 | Homo sapiens | Nuvisan Phospholipase C panel (PLCB3) | IC50 > 20 µM | IC50 > 20 µM | ||
| PLCD1 | Homo sapiens | Nuvisan Phospholipase C panel (PLCD1) | IC50 > 20 µM | IC50 > 20 µM | ||
| PLCG1 | Homo sapiens | Nuvisan Phospholipase C panel (PLCG1) | IC50 > 20 µM | IC50 > 20 µM | ||
| PLCZ1 | Homo sapiens | Nuvisan Phospholipase C panel (PLCZ1) | IC50 > 20 µM | IC50 > 20 µM |
In cell potency
| Target name | Target information | Species | Assay description | BAY-439 | BAY-163 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PLA2G5 | THP-1 cells (human monocytic cell line), human recombinant protein | Homo sapiens | Cellular PLA2G5 assay (THP-1 cells): Substrate: Bis-BODIPY® FL C11-PC | IC50 = 61 nM | Slide 17 in BAY-439 Inhibitor for PLA2G5.pdf |