Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | prostaglandin-endoperoxide synthase 2 | Starlite/ChEMBL | References |
Mus musculus | prostaglandin-endoperoxide synthase 1 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 1.5 | Ability of compound to cause gastric ulcerogenicity was determined in rats at 5 mg/kg | ChEMBL. | 14761182 |
ED50 (functional) | = 0.01 mg kg-1 day-1 | Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using thetapeutic method; dose administered daily twice | ChEMBL. | 14761182 |
ED50 (functional) | = 0.02 mg kg-1 day-1 | Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using thetapeutic method; dose administered daily once | ChEMBL. | 14761182 |
ED50 (functional) | = 0.1 mg kg-1 day-1 | Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using preventive method; dose administered daily twice | ChEMBL. | 14761182 |
IC50 (binding) | = 0.003 ug ml-1 | In vitro inhibitory activity against prostaglandin G/H synthase 2 using mouse peritoneal macrophage method | ChEMBL. | 14761182 |
IC50 (binding) | = 0.003 ug ml-1 | In vitro inhibitory activity against prostaglandin G/H synthase 2 using mouse peritoneal macrophage method | ChEMBL. | 14761182 |
IC50 (binding) | = 0.0067 ug ml-1 | Inhibition of COX2 in C57BL/6 mouse peritoneal macrophages assessed as reduction in PGE2 formation pre-incubated for 2 hrs before LPS stimulation for 16 hrs followed by arachidonic acid addition and measured after 10 mins in presence of 500 uM aspirin by radio-immuno assay or enzyme-immunoassay | PATENT. | No reference |
IC50 (binding) | = 0.3 ug ml-1 | In vitro inhibitory activity against prostaglandin G/H synthase 1 using mouse peritoneal macrophage method | ChEMBL. | 14761182 |
IC50 (binding) | = 0.3 ug ml-1 | In vitro inhibitory activity against prostaglandin G/H synthase 1 using mouse peritoneal macrophage method | ChEMBL. | 14761182 |
IC50 (binding) | = 1.02 ug ml-1 | Inhibition of COX1 in C57BL/6 mouse peritoneal macrophages assessed as reduction in PGE2 formation pre-incubated for 2 hrs followed by arachidonic acid addition and measured after 10 mins by radio-immuno assay or enzyme-immunoassay | PATENT. | No reference |
Inhibition (functional) | = 47 % | Inhibition of carrageenan-induced rat foot oedema following 3 mg/kg administration. | ChEMBL. | 14761182 |
Selectivity (binding) | = 100 | Selectivity of the compound against COX-2 over COX-1 | ChEMBL. | 14761182 |
Selectivity (binding) | = 100 | Selectivity of the compound against COX-2 over COX-1 | ChEMBL. | 14761182 |
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.