Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Cricetulus griseus | Prokineticin receptor 2 | Starlite/ChEMBL | No references |
Cricetulus griseus | Prokineticin receptor 1 | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma japonicum | ko:K04209 neuropeptide Y receptor, invertebrate, putative | Prokineticin receptor 2 | 391 aa | 329 aa | 28.9 % |
Echinococcus multilocularis | neuropeptide receptor | Prokineticin receptor 2 | 391 aa | 357 aa | 24.6 % |
Schistosoma mansoni | peptide (allatostatin)-like receptor | Prokineticin receptor 2 | 391 aa | 375 aa | 24.0 % |
Echinococcus granulosus | allatostatin A receptor | Prokineticin receptor 2 | 391 aa | 372 aa | 23.1 % |
Onchocerca volvulus | Prokineticin receptor 2 | 391 aa | 321 aa | 27.7 % | |
Echinococcus multilocularis | allatostatin A receptor | Prokineticin receptor 2 | 391 aa | 340 aa | 22.9 % |
Echinococcus multilocularis | thyrotropin releasing hormone receptor | Prokineticin receptor 2 | 391 aa | 379 aa | 21.6 % |
Schistosoma japonicum | ko:K04135 adrenergic receptor, alpha 1a, putative | Prokineticin receptor 2 | 391 aa | 376 aa | 22.6 % |
Echinococcus granulosus | thyrotropin releasing hormone receptor | Prokineticin receptor 2 | 391 aa | 379 aa | 22.2 % |
Echinococcus granulosus | neuropeptide receptor | Prokineticin receptor 2 | 391 aa | 322 aa | 31.1 % |
Schistosoma japonicum | ko:K04134 cholinergic receptor, invertebrate, putative | Prokineticin receptor 2 | 391 aa | 406 aa | 21.9 % |
Onchocerca volvulus | Prokineticin receptor 2 | 391 aa | 330 aa | 20.9 % | |
Echinococcus multilocularis | neuropeptide receptor | Prokineticin receptor 2 | 391 aa | 329 aa | 30.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0312 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0312 | 0.5 | 0.5 |
Loa Loa (eye worm) | NNMT/PNMT/TEMT family protein | 0.0312 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 0.81 nM | BindingDB_Patents: Calcium Mobilization Assay. An aequorin-based luminescent assay for calcium mobilization was used to measure mobilization of intracellular Ca2+ (Bullock et al., Mol Pharmacol 65, 582-588, 2004). Chinese hamster ovary (CHO) cells stably expressing photoprotein aequorin and recombinant PKR1 or PKR2 were tested by this method. Briefly, the cells were charged in Opti-MEM (Invitrogen) containing 8 µM of coelenterazine cp at 37° C. for 2 hours. Cells were detached by brief typsinization and maintained in Hank's Balanced Salt Solution (HBSS) plus 10 mM HEPES (pH7.5) and 0.1% BSA at about 5×105 cells/ml. Luminescence measurements were made using a Berthold luminometer. | ChEMBL. | No reference |
Ki (binding) | = 1.7 nM | BindingDB_Patents: Calcium Mobilization Assay. An aequorin-based luminescent assay for calcium mobilization was used to measure mobilization of intracellular Ca2+ (Bullock et al., Mol Pharmacol 65, 582-588, 2004). Chinese hamster ovary (CHO) cells stably expressing photoprotein aequorin and recombinant PKR1 or PKR2 were tested by this method. Briefly, the cells were charged in Opti-MEM (Invitrogen) containing 8 µM of coelenterazine cp at 37° C. for 2 hours. Cells were detached by brief typsinization and maintained in Hank's Balanced Salt Solution (HBSS) plus 10 mM HEPES (pH7.5) and 0.1% BSA at about 5×105 cells/ml. Luminescence measurements were made using a Berthold luminometer. | ChEMBL. | No reference |
Ki (binding) | = 10.4 nM | BindingDB_Patents: Calcium Mobilization Assay. An aequorin-based luminescent assay for calcium mobilization was used to measure mobilization of intracellular Ca2+ (Bullock et al., Mol Pharmacol 65, 582-588, 2004). Chinese hamster ovary (CHO) cells stably expressing photoprotein aequorin and recombinant PKR1 or PKR2 were tested by this method. Briefly, the cells were charged in Opti-MEM (Invitrogen) containing 8 uM of coelenterazine cp at 37degrees C. for 2 hours. Cells were detached by brief typsinization and maintained in Hank's Balanced Salt Solution (HBSS) plus 10 mM HEPES (pH7.5) and 0.1% BSA at about 5x105 cells/ml. Luminescence measurements were made using a Berthold luminometer. | ChEMBL. | No reference |
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.