| Assay Method Information | |
| | Enzyme Inhibitory Assay |
| Description: | The activity of the compounds according to the present invention to inhibit the PARP-1 enzyme was examined using a PARP Assay kit (4671-096-K) purchased from Trevigen. The assay was performed following a modified previously reported method by Lee et al [Methods Find, Exp. Clin. Pharmacol., 27, 617-622, 2005].Histone was coated on 384-well plate, which is a small volume PS plate (784101) of Greiner Bio-One, and left at 25 C. for 2 hours. After that, the plate was rinsed four times with PBS (7.5 mM Na2HPO4, 2.5 mM NaH2PO4, 145 mM NaCl, pH 7.4), and in order to prevent non-specific reaction, the Strep-diluent (provided from kit of Trevigen) was added and left at 25 C. for one hour. After one hour, the plate was again rinsed with PBS four times, and the compounds of the Examples in various concentrations were put into reactant containing PARP-1 enzyme (0.12 unit/well), 2x PARP cocktail. |
| Affinity data for this assay | |
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