Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Delta opioid receptor | Starlite/ChEMBL | References |
Mus musculus | opioid receptor, mu 1 | Starlite/ChEMBL | References |
Rattus norvegicus | Mu opioid receptor | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus multilocularis | tm gpcr rhodopsin gpcr rhodopsin superfamily | Get druggable targets OG5_139759 | All targets in OG5_139759 |
Echinococcus granulosus | tm gpcr rhodopsin | Get druggable targets OG5_139759 | All targets in OG5_139759 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | thyrotropin releasing hormone receptor | Delta opioid receptor | 372 aa | 330 aa | 24.5 % |
Onchocerca volvulus | Delta opioid receptor | 372 aa | 316 aa | 26.9 % | |
Onchocerca volvulus | Delta opioid receptor | 372 aa | 344 aa | 22.1 % | |
Onchocerca volvulus | Programmed cell death protein 5 homolog | Mu opioid receptor | 398 aa | 323 aa | 24.1 % |
Schistosoma japonicum | ko:K04135 adrenergic receptor, alpha 1a, putative | Mu opioid receptor | 398 aa | 397 aa | 22.7 % |
Brugia malayi | ORL1-like opioid receptor | Delta opioid receptor | 372 aa | 300 aa | 24.7 % |
Onchocerca volvulus | Delta opioid receptor | 372 aa | 386 aa | 22.8 % | |
Schistosoma mansoni | peptide (allatostatin)-like receptor | Delta opioid receptor | 372 aa | 353 aa | 29.2 % |
Brugia malayi | GnHR receptor homolog | Delta opioid receptor | 372 aa | 313 aa | 18.5 % |
Echinococcus granulosus | allatostatin A receptor | Delta opioid receptor | 372 aa | 302 aa | 27.8 % |
Schistosoma japonicum | ko:K04134 cholinergic receptor, invertebrate, putative | Delta opioid receptor | 372 aa | 320 aa | 25.6 % |
Schistosoma japonicum | ko:K04209 neuropeptide Y receptor, invertebrate, putative | Delta opioid receptor | 372 aa | 315 aa | 28.6 % |
Echinococcus multilocularis | allatostatin A receptor | Delta opioid receptor | 372 aa | 302 aa | 28.5 % |
Schistosoma mansoni | peptide (FMRFamide/somatostatin)-like receptor | Delta opioid receptor | 372 aa | 366 aa | 22.7 % |
Echinococcus multilocularis | thyrotropin releasing hormone receptor | Delta opioid receptor | 372 aa | 330 aa | 24.2 % |
Schistosoma mansoni | neuropeptide F-like receptor | Mu opioid receptor | 398 aa | 335 aa | 20.6 % |
Loa Loa (eye worm) | neuropeptide F receptor | Delta opioid receptor | 372 aa | 317 aa | 23.3 % |
Schistosoma japonicum | Rhodopsin, putative | Mu opioid receptor | 398 aa | 328 aa | 23.2 % |
Onchocerca volvulus | Mitochondrial inner membrane protein homolog | Mu opioid receptor | 398 aa | 334 aa | 23.1 % |
Onchocerca volvulus | Delta opioid receptor | 372 aa | 353 aa | 21.0 % | |
Onchocerca volvulus | Delta opioid receptor | 372 aa | 349 aa | 22.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0143 | 0.1687 | 0.1687 |
Onchocerca volvulus | 0.0143 | 0.1687 | 0.5764 | |
Brugia malayi | PAS domain containing protein | 0.0067 | 0.0416 | 0.0416 |
Brugia malayi | aryl hydrocarbon receptor AHR-1 | 0.0126 | 0.14 | 0.14 |
Echinococcus granulosus | tm gpcr rhodopsin | 0.0634 | 0.983 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0644 | 1 | 1 |
Echinococcus multilocularis | transfer RNA-Lys | 0.0049 | 0.0129 | 0.0131 |
Echinococcus multilocularis | aryl hydrocarbon receptor | 0.0144 | 0.1696 | 0.1726 |
Loa Loa (eye worm) | hypothetical protein | 0.0126 | 0.141 | 0.141 |
Schistosoma mansoni | hypothetical protein | 0.0225 | 0.3053 | 1 |
Echinococcus granulosus | jun protein | 0.0277 | 0.3915 | 0.3983 |
Echinococcus granulosus | single minded 2 | 0.0049 | 0.0129 | 0.0131 |
Echinococcus granulosus | geminin | 0.0185 | 0.2388 | 0.243 |
Echinococcus multilocularis | geminin | 0.0185 | 0.2388 | 0.243 |
Loa Loa (eye worm) | hypothetical protein | 0.027 | 0.3789 | 0.3789 |
Brugia malayi | hypothetical protein | 0.0218 | 0.2927 | 0.2927 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription factor | 0.0277 | 0.3915 | 0.3983 |
Echinococcus multilocularis | jun protein | 0.0277 | 0.3915 | 0.3983 |
Echinococcus multilocularis | tm gpcr rhodopsin gpcr rhodopsin superfamily | 0.0634 | 0.983 | 1 |
Brugia malayi | bZIP transcription factor family protein | 0.0277 | 0.3915 | 0.3915 |
Onchocerca volvulus | 0.0218 | 0.2927 | 1 | |
Schistosoma mansoni | single-minded | 0.0067 | 0.0416 | 0.1362 |
Schistosoma mansoni | aryl hydrocarbon receptor | 0.0193 | 0.2514 | 0.8234 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription factor | 0.0277 | 0.3915 | 0.3983 |
Loa Loa (eye worm) | hypothetical protein | 0.0126 | 0.14 | 0.14 |
Schistosoma mansoni | hypothetical protein | 0.0185 | 0.2388 | 0.7824 |
Mycobacterium ulcerans | putative regulatory protein | 0.0049 | 0.0129 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0185 | 0.2388 | 0.7824 |
Onchocerca volvulus | 0.005 | 0.0139 | 0.0473 | |
Schistosoma mansoni | jun-related protein | 0.0225 | 0.3053 | 1 |
Brugia malayi | bHLH-PAS transcription factor | 0.0049 | 0.0129 | 0.0129 |
Echinococcus granulosus | aryl hydrocarbon receptor | 0.0144 | 0.1696 | 0.1726 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Emax (functional) | = 134 % | Agonist activity at mu opioid receptor in rat brain assessed as maximal stimulation of [35S]GTPgammaS binding relative to basal level | ChEMBL. | 18062664 |
Emax (functional) | = 134 % | Agonist activity at mu opioid receptor in rat brain assessed as maximal stimulation of [35S]GTPgammaS binding relative to basal level | ChEMBL. | 18062664 |
Emax (functional) | = 322 % | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding relative to basal level | ChEMBL. | 18062664 |
Emax (functional) | = 322 % | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding relative to basal level | ChEMBL. | 18062664 |
IC50 (functional) | = 49.81 nM | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | ChEMBL. | 18062664 |
IC50 (functional) | = 49.81 nM | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | ChEMBL. | 18062664 |
Ki (binding) | = 29.3 pM | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain after 45 mins | ChEMBL. | 18062664 |
Ki (binding) | = 29.3 pM | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain after 45 mins | ChEMBL. | 18062664 |
Ki (binding) | > 10000 pM | Displacement of [3H]deltorphin 2 from delta opioid receptor in Wistar rat brain after 45 mins | ChEMBL. | 18062664 |
Ki (binding) | > 10000 pM | Displacement of [3H]deltorphin 2 from delta opioid receptor in Wistar rat brain after 45 mins | ChEMBL. | 18062664 |
Log10ED50 (functional) | = 6.74 | Agonist activity at mu opioid receptor in rat brain assessed as maximal stimulation of [35S]GTPgammaS binding | ChEMBL. | 18062664 |
Log10ED50 (functional) | = 6.88 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding | ChEMBL. | 18062664 |
Ratio Ki (binding) | > 350 | Selectivity for mu opioid receptor over delta opiod receptor in Wistar rat brain | ChEMBL. | 18062664 |
t1/2 (ADMET) | > 24 hr | Stability in rat brain assessed as half life | ChEMBL. | 18062664 |
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.