Assay Report Card

Basic Information

ID: ALA3706279

Type: Binding

Description: Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues.

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
316.362.562.56
294.353.273.27
277.322.952.95
266.091.831.83