Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | retinoic acid receptor, gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, beta | Starlite/ChEMBL | References |
Homo sapiens | peroxisome proliferator-activated receptor gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, alpha | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, beta | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, alpha | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, gamma | 340 aa | 338 aa | 24.6 % |
Echinococcus granulosus | ecdysone induced protein 78C | peroxisome proliferator-activated receptor gamma | 477 aa | 447 aa | 28.2 % |
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 | 0.0807 | 0.8881 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0516 | 0.1119 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0516 | 0.1119 | 0.5 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.0474 | 0 | 0.5 |
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.0807 | 0.8881 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | 0 nM | In vitro agonistic activity against RXR alpha in CV-1 cells; NC= Not calculated | ChEMBL. | 14592510 |
EC50 (functional) | = 16.3 nM | In vitro agonistic activity against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 16.3 nM | In vitro agonistic activity against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 78 nM | In vitro agonist efficacy against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 78 nM | In vitro agonist efficacy against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
Efficacy (functional) | = 5 nM | In vitro agonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 5 nM | In vitro agonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 83 nM | In vitro anatagonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 83 nM | In vitro anatagonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
IC50 (functional) | = 57.9 nM | In vitro anatagonist activity against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
IC50 (functional) | = 57.9 nM | In vitro anatagonist activity against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 6.1 nM | Binding affinity against RXR alpha receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 6.1 nM | Binding affinity against RXR alpha receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 12.3 nM | Displacement of [3H]-9-cis-RA from RXR beta receptor in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 12.3 nM | Displacement of [3H]-9-cis-RA from RXR beta receptor in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 22.5 nM | Binding affinity against RXR gamma receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 22.5 nM | Binding affinity against RXR gamma receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 2612 nM | Binding affinity against RAR beta receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 2612 nM | Binding affinity against RAR beta receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 4659 nM | Binding affinity against RAR alpha receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 4659 nM | Binding affinity against RAR alpha receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | > 10000 nM | Binding affinity against RAR gamma receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | > 10000 nM | Binding affinity against RAR gamma receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Synergy (functional) | = 1 nM | Agonist synergy against RAR alpha was tested along with 3 nM TTNPB | ChEMBL. | 14592510 |
Synergy (functional) | = 1 nM | Agonist synergy against RAR alpha was tested along with 3 nM TTNPB | ChEMBL. | 14592510 |
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.