Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | retinoic acid receptor, gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, alpha | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | nuclear hormone receptor | 0.0266 | 0.9241 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.014 | 0.0759 | 0.5 |
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.0266 | 0.9241 | 1 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.0129 | 0 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.014 | 0.0759 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | 0 nM | Effective concentration required for agonistic activity in CV-1 cells expressing RXR-alpha; ND means no data | ChEMBL. | 15125928 |
EC50 (functional) | = 4154 nM | Effective concentration for antagonistic activity against RXR-alpha expressed in CV-1 cells | ChEMBL. | 15125928 |
EC50 (functional) | = 4154 nM | Effective concentration for antagonistic activity against RXR-alpha expressed in CV-1 cells | ChEMBL. | 15125928 |
Efficacy (functional) | = 1.78 % | Agonistic efficacy in CV-1 cells (LGD1069 was used as reference) | ChEMBL. | 15125928 |
Efficacy (functional) | = 1.78 % | Agonistic efficacy in CV-1 cells (LGD1069 was used as reference) | ChEMBL. | 15125928 |
Efficacy (functional) | = 48 % | Antagonistic efficacy in CV-1 cells (LGD1069 was used as reference) | ChEMBL. | 15125928 |
Efficacy (functional) | = 48 % | Antagonistic efficacy in CV-1 cells (LGD1069 was used as reference) | ChEMBL. | 15125928 |
Ki (binding) | = 394.7 nM | Ability to displace [3H]-9-cis-RA from Retinoid X receptor alpha in CV-1 cells | ChEMBL. | 15125928 |
Ki (binding) | = 394.7 nM | Ability to displace [3H]-9-cis-RA from Retinoid X receptor alpha in CV-1 cells | ChEMBL. | 15125928 |
Ki (binding) | > 10000 nM | Ability to displace [3H]-ATRA from Retinoic acid receptor gamma in CV-1 cells | ChEMBL. | 15125928 |
Ki (binding) | > 10000 nM | Ability to displace [3H]-ATRA from Retinoic acid receptor gamma in CV-1 cells | ChEMBL. | 15125928 |
Ratio (functional) | = 123.1 | Ratio between agonistic efficacy in PPAR gamma | ChEMBL. | 15125928 |
Ratio (functional) | = 1481 | Ratio between effective concentrations(Agonist) in PPAR gamma | ChEMBL. | 15125928 |
Ratio (functional) | = 123.1 | Ratio between agonistic efficacy in PPAR gamma | ChEMBL. | 15125928 |
Ratio (functional) | = 1481 | Ratio between effective concentrations(Agonist) in PPAR gamma | ChEMBL. | 15125928 |
Synergy (functional) | = 1.5 | RAR agonist synergy calculated using 3 nM of TTNPB | ChEMBL. | 15125928 |
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.