Assay Report Card

Basic Information

ID: ALA3707489

Type: Binding

Description: Displacement Assay: Affinity evaluation of the tested compounds and their selectivity with respect to the different PARP isoforms of interest was assessed in a displacement assay.The identification of compounds capable of binding several PARP proteins is carried out through a screening method including the steps of a) providing a reaction mixture containing: the PARP protein isoform under investigation,a compound of formula (IP). b) comparing the polarization signal generated in the absence of the test compound with the one generated in the presence of different concentrations of the test compound, and c) evaluating the ability of the test compound to displace the compound of formula (IP) as defined above indicated from a decreased fluorescence polarization level. Preferably, for the screening method above cited, both the PARP protein and the 5H-phenanthridin-6-one-derived probe of formula (IP) are pre-mixed, or the PARP protein and the test compound are pre-mixed.

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
278.290.490.49
292.310.500.50
374.462.552.55