Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | RAR-related orphan receptor gamma | References | |
Homo sapiens | RAR-related orphan receptor C | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 0.029 uM | Inhibition of mouse RORgamma ligand binding domain (Isoleucine 251 to Lysine 516) expressed in CHOK1 cells incubated for 2 days by Gal4 luciferase reporter gene assay | ChEMBL. | 26819660 |
EC50 (binding) | = 0.034 uM | Inhibition of human RORgamma ligand binding domain (Serine 253 to Lysine 518 residues) expressed in CHOK1 cells incubated for 2 days by Gal4 luciferase reporter gene assay | ChEMBL. | 26819660 |
EC50 (binding) | = 0.2 uM | Inhibition of human GST-tagged RORgamma ligand binding domain (253 to 518 residues) expressed in sf9 cells using biotin-EEPSLLKKLLLAPA by FRET assay | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human FXR | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of mouse GR | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human RORalpha | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human SF-1 receptor | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of mouse LXRalpha | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human PPARgamma | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human RARalpha | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human RXRalpha | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human VDR | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human PPARalpha | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human RARbeta | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human PPARdelta | ChEMBL. | 26819660 |
EC50 (binding) | > 20 uM | Inhibition of human RORbeta | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP1A2 in human liver microsomes using ethoxyresorufin as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP2A6 in human liver microsomes using coumarin as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
Inhibition (ADMET) | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated with substrate for 5 mins followed by NADPH addition measured after 20 mins by HPLC analysis | ChEMBL. | 26819660 |
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.