Potency data for probe BAY-390 and control BAY-9897
In cell potency
| Target name | Target information | Species | Assay description | Probe result (SD) | Control result (SD) | Publication of assay conditions |
|---|---|---|---|---|---|---|
| TRPA1 | TRPA1 overexpressing cell line (e.g. CHO hTRPA1 GCaMP6) | Homo sapiens | FLIPR Ca2+ assay (human TRAP1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 16 nM | IC50 > 25 µM | |
| TRPA1 | TRPA1 overexpressing cell line (CHO or HEK cells) | Rattus sp. | FLIPR Ca2+ assay (rat TRPA1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 63 nM | IC50 > 25 µM | |
| TRPA1 | TRPA1 overexpressing cell line (CHO or HEK cells) | Mus musculus | FLIPR Ca2+ assay (mouse TRPA1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 73 nM | ||
| TRPA1 | TRPA1 overexpressing cell line (CHO or HEK cells) | Cavia porcellus | FLIPR Ca2+ assay (guinea pig TRPA1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 68 nM | ||
| TRPA1 | TRPA1 overexpressing cell line (CHO or HEK cells) | Canis lupus familiaris | FLIPR Ca2+ assay (dog TRPA1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 81 nM | ||
| TRPA1 | TRPA1 overexpressing cell line (CHO or HEK cells) | Pan troglodytes | FLIPR Ca2+ assay (monkey TRPA1): Activation with agonist supercinnemaldehyde (SCA), probe added for 10 min, Readout: calcium sensor GCaMP6 (or Fluo8) | IC50 = 19 nM | ||
| TRPA1 | Homo sapiens | Ephys (human TRPA1) | IC50 = 82 nM | |||
| TRPV1 | Homo sapiens | TRP selectivity screen (TRPV1) | IC50 > 25 µM | IC50 > 25 µM | ||
| TRPV4 | Homo sapiens | TRP selectivity screen (TRPV4) | IC50 > 25 µM | IC50 > 25 µM | ||
| TRPC3 | Homo sapiens | TRP selectivity screen (TRPC3) | IC50 > 25 µM | |||
| TRPC5 | Homo sapiens | TRP selectivity screen (TRPC5) | IC50 = 5.600 µM | IC50 = 10 µM | ||
| TRPC6 | Homo sapiens | TRP selectivity screen (TRPC6) | IC50 > 25 µM | IC50 > 30 µM | ||
| KCNK9 | Homo sapiens | Selectivity screen (KCNK9) | IC50 > 25 µM | |||
| CACNA1H | Homo sapiens | Selectivity screen (CACNA1H) | IC50 > 30 µM |