Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Cannabinoid CB2 receptor | Starlite/ChEMBL | References |
Homo sapiens | cannabinoid receptor 2 (macrophage) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma japonicum | ko:K04135 adrenergic receptor, alpha 1a, putative | Cannabinoid CB2 receptor | 360 aa | 370 aa | 23.8 % |
Schistosoma japonicum | ko:K04134 cholinergic receptor, invertebrate, putative | Cannabinoid CB2 receptor | 360 aa | 360 aa | 23.1 % |
Schistosoma japonicum | ko:K04209 neuropeptide Y receptor, invertebrate, putative | Cannabinoid CB2 receptor | 360 aa | 311 aa | 20.6 % |
Schistosoma mansoni | biogenic amine (5HT) receptor | Cannabinoid CB2 receptor | 360 aa | 370 aa | 23.5 % |
Schistosoma mansoni | peptide (allatostatin)-like receptor | Cannabinoid CB2 receptor | 360 aa | 323 aa | 22.6 % |
Echinococcus multilocularis | neuropeptide receptor | Cannabinoid CB2 receptor | 360 aa | 299 aa | 24.7 % |
Echinococcus granulosus | neuropeptide receptor | Cannabinoid CB2 receptor | 360 aa | 337 aa | 24.0 % |
Onchocerca volvulus | Cannabinoid CB2 receptor | 360 aa | 389 aa | 21.1 % | |
Loa Loa (eye worm) | neuropeptide F receptor | Cannabinoid CB2 receptor | 360 aa | 348 aa | 24.7 % |
Onchocerca volvulus | Cannabinoid CB2 receptor | 360 aa | 327 aa | 19.6 % | |
Echinococcus multilocularis | allatostatin A receptor | Cannabinoid CB2 receptor | 360 aa | 342 aa | 22.8 % |
Schistosoma mansoni | opsin-like receptor | Cannabinoid CB2 receptor | 360 aa | 314 aa | 22.0 % |
Onchocerca volvulus | Cannabinoid CB2 receptor | 360 aa | 330 aa | 20.9 % | |
Echinococcus granulosus | allatostatin A receptor | Cannabinoid CB2 receptor | 360 aa | 363 aa | 22.9 % |
Onchocerca volvulus | Cannabinoid CB2 receptor | 360 aa | 297 aa | 21.9 % | |
Onchocerca volvulus | Phospholipase d-related homolog | Cannabinoid CB2 receptor | 360 aa | 309 aa | 23.3 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 15.9 nM | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding after 30 mins by scintillation proximity assay | ChEMBL. | 23795771 |
EC50 (functional) | > 100000 nM | Agonist activity at human CB1 receptor expressed in Sf9 cells assessed as stimulation of [35S]GTPgamma binding incubated for 15 mins prior to [35S]GTPgamma addition measured after 35 mins by scintillation proximity assay | ChEMBL. | 23795771 |
Efficacy (functional) | = 90.7 % | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding after 30 mins by scintillation proximity assay relative to methanandamide | ChEMBL. | 23795771 |
Ki (binding) | = 87.1 nM | Displacement of [3H]-CP-55940 from rat CB2 receptor expressed in CHO cells after 90 mins | ChEMBL. | 23795771 |
Ki (binding) | = 104 nM | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in CHO cells after 90 mins | ChEMBL. | 23795771 |
Stabilty (ADMET) | = 18 % | Metabolic stability in human liver microsomes assessed as compound remaining at 4 uM after 30 mins by LC-ESI/MS analysis | ChEMBL. | 23795771 |
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.