Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | peroxisome proliferator-activated receptor delta | Starlite/ChEMBL | References |
Mus musculus | peroxisome proliferator activator receptor delta | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | peroxisome proliferator-activated receptor delta | 441 aa | 369 aa | 24.7 % |
Brugia malayi | ecdysteroid receptor | peroxisome proliferator activator receptor delta | 440 aa | 364 aa | 26.1 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Antagonist activity at PPARgamma in mouse NIH3T3 cells coexpressing LexA assessed as decrease in GW1929-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay relative to control | ChEMBL. | 22369181 | |
Activity (functional) | Antagonist activity at PPARbeta/delta in mouse NIH3T3 cells coexpressing LexA assessed as decrease in L165,041-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay relative to control | ChEMBL. | 22369181 | |
Activity (functional) | Antagonist activity at PPARalpha in mouse NIH3T3 cells coexpressing LexA assessed as decrease in GW7647-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay relative to control | ChEMBL. | 22369181 | |
Activity (binding) | Displacement of fluormone Pan-PPAR Green from mouse recombinant GST-tagged PPARbeta/delta LBD at 1 uM after 60 mins by TR-FRET assay | ChEMBL. | 22369181 | |
Activity (binding) | Displacement of fluormone Pan-PPAR Green from PPARalpha at 100 to 1000 nM after 60 mins by TR-FRET assay | ChEMBL. | 22369181 | |
Activity (binding) | Displacement of fluormone Pan-PPAR Green from PPARgamma at 100 to 1000 nM after 60 mins by TR-FRET assay | ChEMBL. | 22369181 | |
Activity (functional) | Inverse agonist activity at GST-tagged recombinant mouse PPARbeta/delta assessed as increase in corepressor peptide SMRT-ID2 interaction after 60 mins by TR-FRET assay | ChEMBL. | 22369181 | |
IC50 (functional) | = 9.5 nM | Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis | ChEMBL. | 22369181 |
IC50 (binding) | = 26.9 nM | Displacement of fluormone Pan-PPAR Green from mouse recombinant GST-tagged PPARbeta/delta LBD after 60 mins by TR-FRET assay | ChEMBL. | 22369181 |
IC50 (binding) | = 29 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 20 mins by TR-FRET assay | ChEMBL. | 26707845 |
IC50 (binding) | = 30.4 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 40 mins by TR-FRET assay | ChEMBL. | 26707845 |
IC50 (binding) | = 32.7 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 1 hr by TR-FRET assay | ChEMBL. | 26707845 |
IC50 (binding) | = 37 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 2 hrs by TR-FRET assay | ChEMBL. | 26707845 |
IC50 (binding) | = 40.1 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 3 hrs by TR-FRET assay | ChEMBL. | 26707845 |
IC50 (binding) | = 48 nM | Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 24 hrs by TR-FRET assay | ChEMBL. | 26707845 |
Inhibition (binding) | Inhibition of wild type PPARD-mediated downregulation of Angptl expression in mouse macrophages at 1 uM after 6 hrs by RT-qPCR analysis | ChEMBL. | 22369181 | |
Inhibition (functional) | Inverse agonist activity at PPARbeta/delta in human WPMY-1 cells assessed as increase in HDAC3 recruitment to ANGPTL4 at 1 uM after 30 mins by chromatin immune precipitation analysis | ChEMBL. | 22369181 | |
T1/2 (ADMET) | = 76 min | Half life in CD1 mouse plasma at 1 mg/kg, iv | ChEMBL. | 22369181 |
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.
2 literature references were collected for this gene.