Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | estrogen receptor 2 (ER beta) | Starlite/ChEMBL | References |
Homo sapiens | androgen receptor | Starlite/ChEMBL | References |
Homo sapiens | estrogen receptor 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | estrogen receptor 2 (ER beta) | 495 aa | 418 aa | 25.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Entamoeba histolytica | geranylgeranyl pyrophosphate synthetase, putative | 0.0114 | 0.0582 | 0.5 |
Mycobacterium ulcerans | geranylgeranyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Schistosoma mansoni | lipoxygenase | 0.0133 | 0.1118 | 0.1118 |
Echinococcus granulosus | arachidonate 5 lipoxygenase | 0.0133 | 0.1118 | 0.0569 |
Schistosoma mansoni | glutathione synthetase | 0.0114 | 0.0582 | 0.0582 |
Plasmodium falciparum | geranylgeranyl pyrophosphate synthase, putative | 0.0451 | 1 | 1 |
Chlamydia trachomatis | geranylgeranyl pyrophosphate synthase | 0.0114 | 0.0582 | 0.5 |
Leishmania major | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Trichomonas vaginalis | geranylgeranyl pyrophosphate synthase, putative | 0.0451 | 1 | 0.5 |
Echinococcus granulosus | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Treponema pallidum | octaprenyl-diphosphate synthase | 0.0114 | 0.0582 | 0.5 |
Entamoeba histolytica | bifunctional short chain isoprenyl diphosphate synthase, putative | 0.0114 | 0.0582 | 0.5 |
Schistosoma mansoni | geranylgeranyl pyrophosphate synthase | 0.0114 | 0.0582 | 0.0582 |
Mycobacterium tuberculosis | Probable geranylgeranyl pyrophosphate synthetase IdsA2 (ggppsase) (GGPP synthetase) (geranylgeranyl diphosphate synthase) | 0.0451 | 1 | 1 |
Entamoeba histolytica | geranylgeranyl pyrophosphate synthase, putative | 0.0114 | 0.0582 | 0.5 |
Mycobacterium leprae | PROBABLE POLYPRENYL-DIPHOSPHATE SYNTHASE GRCC1 (POLYPRENYL PYROPHOSPHATE SYNTHETASE) | 0.0114 | 0.0582 | 0.5 |
Echinococcus multilocularis | arachidonate 5 lipoxygenase | 0.0133 | 0.1118 | 0.0569 |
Trypanosoma cruzi | farnesyl pyrophosphate synthase, putative | 0.0451 | 1 | 1 |
Trichomonas vaginalis | geranylgeranyl pyrophosphate synthase, putative | 0.0451 | 1 | 0.5 |
Echinococcus multilocularis | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Trichomonas vaginalis | geranylgeranyl diphosphate synthase, putative | 0.0451 | 1 | 0.5 |
Trypanosoma brucei | RNA helicase, putative | 0.0297 | 0.5692 | 0.5426 |
Plasmodium vivax | geranylgeranyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Trypanosoma brucei | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Schistosoma mansoni | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Giardia lamblia | Farnesyl diphosphate synthase | 0.0451 | 1 | 0.5 |
Trypanosoma cruzi | farnesyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Wolbachia endosymbiont of Brugia malayi | geranylgeranyl pyrophosphate synthase | 0.0114 | 0.0582 | 0.5 |
Toxoplasma gondii | polyprenyl synthetase superfamily protein | 0.0451 | 1 | 1 |
Loa Loa (eye worm) | polyprenyl synthetase | 0.0451 | 1 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0297 | 0.5692 | 0.5692 |
Wolbachia endosymbiont of Brugia malayi | geranylgeranyl pyrophosphate synthase | 0.0114 | 0.0582 | 0.5 |
Mycobacterium ulcerans | geranylgeranyl pyrophosphate synthase | 0.0451 | 1 | 1 |
Schistosoma mansoni | trans-prenyltransferase | 0.0114 | 0.0582 | 0.0582 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 379 nM | Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERbeta | ChEMBL. | 16309907 |
EC50 (functional) | = 379 nM | Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERbeta | ChEMBL. | 16309907 |
EC50 (functional) | > 1000 nM | Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERalpha | ChEMBL. | 16309907 |
EC50 (functional) | > 1000 nM | Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERalpha | ChEMBL. | 16309907 |
IC50 (binding) | = 7.9 nM | Inhibitory activity against AR | ChEMBL. | 16309907 |
IC50 (binding) | = 7.9 nM | Inhibitory activity against AR | ChEMBL. | 16309907 |
IC50 (binding) | = 782 nM | Binding affinity to human ERbeta | ChEMBL. | 16309907 |
IC50 (binding) | = 782 nM | Binding affinity to human ERbeta | ChEMBL. | 16309907 |
IC50 (binding) | > 10000 nM | Binding affinity to human ERalpha | ChEMBL. | 16309907 |
IC50 (binding) | > 10000 nM | Binding affinity to human ERalpha | ChEMBL. | 16309907 |
Ratio EC50 (functional) | > 2.6 | Selectivity for transactivation of ALP gene expression in HEK293 cells transfected with hERbeta over hERalpha | ChEMBL. | 16309907 |
Ratio EC50 (functional) | > 2.6 | Selectivity for transactivation of ALP gene expression in HEK293 cells transfected with hERbeta over hERalpha | ChEMBL. | 16309907 |
Ratio IC50 (binding) | > 12 | Selectivity for human ERbeta over ERalpha | ChEMBL. | 16309907 |
Ratio IC50 (binding) | = 0.01 | Selectivity for human ERbeta over AR | ChEMBL. | 16309907 |
Ratio IC50 (binding) | > 12 | Selectivity for human ERbeta over ERalpha | ChEMBL. | 16309907 |
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.