Potency data for probe JYQ-173 and control MB078
In vitro potency
| Target name | Target information | Species | Assay description | JYQ-173 | MB078 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PARK7 | GST recombinant human protein | Homo sapiens | DiFMUAc assay (PARK7): Activity assay that relies on the deacetylation of the fluorogenic substrate 6,8-difluoro-4-methylumbelliferyl (DiFMUAc). Irreversible covalent binding to Cys106. | kinact/KIapp = 12093 M-1s-1 (n=3) | IC50 = 2.24 µM (n=3) | PMID: 38713163 |
| PARK7 | GST recombinant human protein | Homo sapiens | Fluorescence Polarization assay (PARK7) | IC50 = 100 nM (n=3) | IC50 = 3.6 µM (n=3) | PMID: 36149939 |
| UCHL1 | recombinant human protein | Homo sapiens | UCHL1 inhibition assay with Ub-Rho-morpholine as substrate | IC50 = 18.96 µM | PMID: 32886496 |
In cell potency
| Target name | Target information | Species | Assay description | JYQ-173 | MB078 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PARK7 | HEK293 cells | Homo sapiens | ABPP assay (PARK7): Activity based protein profiling assay; 1h, 37 °C | Full inhibition < 1 µM |