Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | peroxisome proliferator-activated receptor gamma | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | ecdysone induced protein 78C | peroxisome proliferator-activated receptor gamma | 477 aa | 447 aa | 28.2 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 5.97 uM hr | Dose-normalized AUC was determined in rat after peroral administration of the compound (2 mg/kg) | ChEMBL. | 12729668 |
Clp (ADMET) | = 3.6 ml min-1 kg-1 | Plasma clearance was determined in rat after intravenous administion of the compound (0.5 mg/kg) | ChEMBL. | 12729668 |
EC50 (binding) | Binding affinity to human PPAR alpha | ChEMBL. | 16384704 | |
EC50 (binding) | Binding affinity to human PPAR delta | ChEMBL. | 16384704 | |
EC50 (functional) | Transactivation by human PPAR delta in COS1 cells | ChEMBL. | 16384704 | |
EC50 (functional) | Transactivation by human PPAR alpha in COS1 cells | ChEMBL. | 16384704 | |
EC50 (binding) | 0 | Binding affinity to human PPAR alpha | ChEMBL. | 16384704 |
EC50 (binding) | 0 | Binding affinity to human PPAR delta | ChEMBL. | 16384704 |
EC50 (functional) | 0 | Transactivation by human PPAR alpha in COS1 cells | ChEMBL. | 16384704 |
EC50 (functional) | 0 | Transactivation by human PPAR delta in COS1 cells | ChEMBL. | 16384704 |
EC50 (functional) | = 80 nM | Transactivation by human PPAR gamma in COS1 cells | ChEMBL. | 16384704 |
EC50 (functional) | = 80 nM | Transactivation by human PPAR gamma in COS1 cells | ChEMBL. | 16384704 |
EC50 (binding) | = 735 nM | Binding affinity to human PPAR gamma | ChEMBL. | 16384704 |
EC50 (binding) | = 735 nM | Binding affinity to human PPAR gamma | ChEMBL. | 16384704 |
EC50 (functional) | = 0.06 uM | In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells | ChEMBL. | 12729668 |
EC50 (functional) | = 0.06 uM | In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells | ChEMBL. | 12729668 |
EC50 (binding) | = 0.06 uM | Transactivation activity at Homo sapiens (human) PPARgamma | ChEMBL. | No reference |
EC50 (functional) | > 50 uM | In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells | ChEMBL. | 12729668 |
EC50 (functional) | > 50 uM | In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells | ChEMBL. | 12729668 |
EC50 (functional) | > 50 uM | In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells | ChEMBL. | 12729668 |
EC50 (functional) | > 50 uM | In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells | ChEMBL. | 12729668 |
F (ADMET) | = 63 % | Oral bioavailability in rat (dose 2 mg/kg) | ChEMBL. | 12729668 |
Glucose correction (functional) | = 78 % | In vivo glucose correction was determined in male db/db mice after administration at 10 mg/kg | ChEMBL. | 12729668 |
IC50 (binding) | = 0.82 uM | In vitro binding affinity against human PPAR gamma (peroxisome proliferator-activated gamma receptor) | ChEMBL. | 12729668 |
IC50 (binding) | = 0.82 uM | In vitro binding affinity against human PPAR gamma (peroxisome proliferator-activated gamma receptor) | ChEMBL. | 12729668 |
IC50 (binding) | > 50 uM | In vitro binding affinity against human PPAR alpha (peroxisome proliferator-activated alpha receptor) | ChEMBL. | 12729668 |
IC50 (binding) | > 50 uM | In vitro binding affinity against human PPAR delta (peroxisome proliferator-activated delta receptor) | ChEMBL. | 12729668 |
IC50 (binding) | > 50 uM | In vitro binding affinity against human PPAR alpha (peroxisome proliferator-activated alpha receptor) | ChEMBL. | 12729668 |
IC50 (binding) | > 50 uM | In vitro binding affinity against human PPAR delta (peroxisome proliferator-activated delta receptor) | ChEMBL. | 12729668 |
T1/2 (ADMET) | = 2.1 hr | Half-life was determined in rat after intravenous administion of the compound (0.5 mg/kg) | ChEMBL. | 12729668 |
Triglyceride correction (functional) | = 71 % | In vivo triglyceride correction was determined in male db/db mice after administration at 10 mg/kg | ChEMBL. | 12729668 |
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.