| Assay Method Information | |
| | Biochemical Assay |
| Description: | In these experiments, compounds from Example 1 were evaluated in a biochemical assay to characterize ligand binding to TLX by detecting alterations in the ability of the TLX ligand binding domain to recruit an NR box peptide derived from the nuclear receptor-interacting protein 1 (NRIP1; receptor-interacting protein 140 (RIP140) transcriptional cofactor. RIP140 has been previously identified as a TLX interacting protein. AlphaScreen (Perkin Elmer, Shelton, CT) technology was used to detect the TLX-RIP140 NR box peptide interaction. The AlphaScreen assay was performed as previously described using other nuclear receptors including ROR, FXR, LXR, VDR and RXR. The present experiments used the N-terminal his-tagged ligand-binding domain (LBD) of TLX (NovAliX SAS, Strasbourg, France) and an N-terminal biotinylated RIP140-L6 peptide with a N-terminal KGG linker, namely (KGGQDTSKNSKLNSHQKVTLLQLLLGHKNEENV (aa484-513)). |
| Affinity data for this assay | |
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