| Assay Method Information | |
| | Fluorescence Polarization (FP) Assays |
| Description: | Compounds of the present disclosure were evaluated for potency and selectivity in a fluorescence polarization (FP) assay that measures inhibition of SMAC peptide binding to ML-IAP. To measure SMAC peptide binding, multi-well plate format FP assays based on the ability of SMAC peptides to bind the BIR domains of several IAPs are used to generate IC50 and Ki values for analogues. The FP assays utilize plasmid constructs encoding various full length IAPs or fragments for expression as either GST or His6-fusion proteins in bacteria. Compounds are evaluated for activity against several members of the IAP family, including the BIR domains of XIAP, cIAP1 and cIAP2 in order to generate selectivity profiles of the compounds disclosed herein. These assays also enable the identification and characterization of potency profiles of ML-IAP binding. |
| Affinity data for this assay | |
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