Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | RAR-related orphan receptor C | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 4.3 uM | Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis | ChEMBL. | 26048793 |
Efficacy (binding) | = -73 % | Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis relative to apo-RORc ligand binding domain | ChEMBL. | 26048793 |
IC50 (binding) | Displacement of fluormone PPARgamma green from GST-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay | ChEMBL. | 26048793 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.