| Assay Method Information | |
| | Inhibition of PARG TEMU Assay |
| Description: | The ability of the compounds of the Examples to inhibit PARG activity in 4. (trifluoromethyl)umbelliferone (TFMU) assay was determined as described below. PARG inhibitors were added into 384 well plate for a 10-point dose response curve at 1:3 dilutions. TFMU PARG substrate and PARG (250 pM or 2 nM) were then added to the plate to initiate enzymatic reaction. After incubation with the reagent, luminescence was read. IC50 values were calculated using set control points for 100% inhibition as no enzyme and 0% inhibition 250 pM or 2 nM of PARG enzyme. |
| Affinity data for this assay | |
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