Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase) | Starlite/ChEMBL | References |
Homo sapiens | prostaglandin-endoperoxide synthase 1 (prostaglandin G/H synthase and cyclooxygenase) | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | cathepsin b | 0.244 | 0.2898 | 1 |
Plasmodium falciparum | plasmepsin IV | 0.0308 | 0 | 0.5 |
Onchocerca volvulus | 0.0308 | 0 | 0.5 | |
Giardia lamblia | Cathepsin B precursor | 0.0805 | 0.0676 | 0.5 |
Plasmodium vivax | plasmepsin IV, putative | 0.0308 | 0 | 0.5 |
Leishmania major | cysteine peptidase C (CPC),CPC cysteine peptidase, Clan CA, family C1, Cathepsin B-like | 0.0805 | 0.0676 | 0.5 |
Plasmodium falciparum | plasmepsin I | 0.0308 | 0 | 0.5 |
Trichomonas vaginalis | Clan CA, family C1, cathepsin B-like cysteine peptidase | 0.0805 | 0.0676 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.244 | 0.2898 | 1 |
Plasmodium vivax | plasmepsin V, putative | 0.0308 | 0 | 0.5 |
Trypanosoma cruzi | cysteine peptidase C (CPC), putative | 0.244 | 0.2898 | 1 |
Plasmodium vivax | aspartyl protease, putative | 0.0308 | 0 | 0.5 |
Plasmodium falciparum | plasmepsin V | 0.0308 | 0 | 0.5 |
Plasmodium falciparum | plasmepsin VI | 0.0308 | 0 | 0.5 |
Plasmodium falciparum | plasmepsin IX | 0.0308 | 0 | 0.5 |
Giardia lamblia | Cathepsin B precursor | 0.0805 | 0.0676 | 0.5 |
Giardia lamblia | Cathepsin B precursor | 0.0805 | 0.0676 | 0.5 |
Plasmodium falciparum | plasmepsin VII | 0.0308 | 0 | 0.5 |
Plasmodium vivax | aspartyl protease, putative | 0.0308 | 0 | 0.5 |
Schistosoma mansoni | cathepsin B-like peptidase (C01 family) | 0.0805 | 0.0676 | 0.0676 |
Echinococcus multilocularis | cathepsin b | 0.244 | 0.2898 | 1 |
Brugia malayi | cathepsin B-like cysteine proteinase | 0.244 | 0.2898 | 1 |
Plasmodium falciparum | plasmepsin III | 0.0308 | 0 | 0.5 |
Toxoplasma gondii | cathepsin B | 0.0805 | 0.0676 | 1 |
Echinococcus granulosus | cathepsin b | 0.244 | 0.2898 | 1 |
Plasmodium falciparum | plasmepsin X | 0.0308 | 0 | 0.5 |
Loa Loa (eye worm) | cathepsin B | 0.0805 | 0.0676 | 0.2333 |
Echinococcus granulosus | cathepsin b | 0.244 | 0.2898 | 1 |
Plasmodium vivax | aspartyl proteinase, putative | 0.0308 | 0 | 0.5 |
Plasmodium vivax | aspartyl proteinase, putative | 0.0308 | 0 | 0.5 |
Plasmodium falciparum | plasmepsin II | 0.0308 | 0 | 0.5 |
Plasmodium falciparum | plasmepsin VIII, putative | 0.0308 | 0 | 0.5 |
Plasmodium vivax | aspartyl protease, putative | 0.0308 | 0 | 0.5 |
Schistosoma mansoni | SmCB2 peptidase (C01 family) | 0.244 | 0.2898 | 0.2898 |
Onchocerca volvulus | 0.0308 | 0 | 0.5 | |
Schistosoma mansoni | cathepsin B-like peptidase (C01 family) | 0.244 | 0.2898 | 0.2898 |
Trypanosoma brucei | cysteine peptidase C (CPC) | 0.0805 | 0.0676 | 0.5 |
Schistosoma mansoni | cathepsin B-like peptidase (C01 family) | 0.244 | 0.2898 | 0.2898 |
Schistosoma mansoni | cathepsin B-like peptidase (C01 family) | 0.244 | 0.2898 | 0.2898 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 44 % | Antiinflammatory activity against Sprague-Dawley rat carrageenan air-pouch model assessed as reduction of prostaglandin E2 at 45 umol/kg, po | ChEMBL. | 17994684 |
Activity (functional) | = 59 % | Antiinflammatory activity against intrapouch dosed Sprague-Dawley rat carrageenan air-pouch model assessed as reduction of prostaglandin E2 at 45 umol/kg | ChEMBL. | 17994684 |
IC50 (binding) | = 1.2 uM | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production | ChEMBL. | 17994684 |
IC50 (binding) | = 1.2 uM | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production | ChEMBL. | 17994684 |
IC50 (binding) | = 11 uM | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production | ChEMBL. | 17994684 |
IC50 (binding) | = 11 uM | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production | ChEMBL. | 17994684 |
Inhibition (binding) | = 7 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 30 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 7 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 30 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 15 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 10 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 15 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 10 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 16 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 100 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 16 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 100 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 20 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 30 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 20 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 30 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 31 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 31 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 57 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 10 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 57 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 10 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 68 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 68 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 72 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 1 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 72 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 1 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 85 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 0.3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 85 % | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 0.3 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 100 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 1 uM relative to control | ChEMBL. | 17994684 |
Inhibition (binding) | = 100 % | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 1 uM relative to control | ChEMBL. | 17994684 |
Ratio IC50 (binding) | = 9.1 | Selectivity for human COX2 over human COX1 | ChEMBL. | 17994684 |
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.