Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | APH1B gamma secretase subunit | Starlite/ChEMBL | References |
Homo sapiens | APH1A gamma secretase subunit | References | |
Homo sapiens | presenilin 1 | References | |
Homo sapiens | presenilin 2 | References | |
Homo sapiens | presenilin enhancer gamma secretase subunit | References | |
Homo sapiens | nicastrin | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | oxalate:formate antiporter | presenilin enhancer gamma secretase subunit | 101 aa | 98 aa | 29.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | kelch ECH associated protein 1 like | 0.0489 | 0.8256 | 0.8256 |
Loa Loa (eye worm) | gamma-secretase subunit pen-2 | 0.0233 | 0.3921 | 0.3921 |
Echinococcus multilocularis | Nicastrin | 0.0121 | 0.2024 | 0.2024 |
Trypanosoma cruzi | Aph-1 protein, putative | 0.0231 | 0.3881 | 0.9136 |
Echinococcus multilocularis | kelch ECH associated protein 1 | 0.0489 | 0.8256 | 0.8256 |
Trypanosoma cruzi | presenilin-like aspartic peptidase, putative | 0.0248 | 0.4179 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0121 | 0.2024 | 0.2024 |
Echinococcus multilocularis | presenilin enhancer 2 | 0.0233 | 0.3921 | 0.3921 |
Loa Loa (eye worm) | presenilin spe-4 | 0.0087 | 0.1447 | 0.1447 |
Echinococcus multilocularis | presenilin | 0.0248 | 0.4179 | 0.4179 |
Brugia malayi | hypothetical protein | 0.0087 | 0.1447 | 0.1447 |
Toxoplasma gondii | hypothetical protein | 0.0087 | 0.1447 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0186 | 0.3129 | 0.6957 |
Schistosoma mansoni | hypothetical protein | 0.0121 | 0.2024 | 0.2024 |
Schistosoma mansoni | gamma-secretase subunit aph-1 | 0.0592 | 1 | 1 |
Brugia malayi | Presenilin spe-4 | 0.0087 | 0.1447 | 0.1447 |
Schistosoma mansoni | hypothetical protein | 0.049 | 0.8279 | 0.8279 |
Echinococcus granulosus | kelch ECH associated protein 1 | 0.0489 | 0.8256 | 0.8256 |
Echinococcus multilocularis | gamma secretase subunit aph 1 | 0.0592 | 1 | 1 |
Echinococcus granulosus | nicalin | 0.0044 | 0.0728 | 0.0728 |
Schistosoma mansoni | subfamily A22A unassigned peptidase (A22 family) | 0.0248 | 0.4179 | 0.4179 |
Brugia malayi | Presenilin-like protein At2g29900 | 0.0087 | 0.1447 | 0.1447 |
Trichomonas vaginalis | Clan AD, family A22, presenilin-like aspartic peptidase | 0.0248 | 0.4179 | 1 |
Trypanosoma cruzi | Aph-1 protein, putative | 0.0231 | 0.3881 | 0.9136 |
Echinococcus multilocularis | kelch ECH associated protein 1 | 0.0489 | 0.8256 | 0.8256 |
Brugia malayi | Presenilin spe-4 | 0.0087 | 0.1447 | 0.1447 |
Entamoeba histolytica | hypothetical protein | 0.0186 | 0.3129 | 0.6957 |
Brugia malayi | Presenilin family protein | 0.0248 | 0.4179 | 0.4179 |
Leishmania major | presenilin-like aspartic peptidase, putative,presenilin-like aspartic peptidase, clan AD, family A22A, putative | 0.0248 | 0.4179 | 1 |
Brugia malayi | gamma-secretase subunit pen-2 | 0.0233 | 0.3921 | 0.3921 |
Echinococcus granulosus | presenilin enhancer 2 | 0.0233 | 0.3921 | 0.3921 |
Brugia malayi | hypothetical protein | 0.0186 | 0.3129 | 0.3129 |
Entamoeba histolytica | hypothetical protein | 0.0186 | 0.3129 | 0.6957 |
Echinococcus granulosus | presenilin | 0.0248 | 0.4179 | 0.4179 |
Entamoeba histolytica | hypothetical protein | 0.0186 | 0.3129 | 0.6957 |
Brugia malayi | hypothetical protein | 0.0121 | 0.2024 | 0.2024 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription | 0.0186 | 0.3129 | 0.3129 |
Trichomonas vaginalis | Clan AD, family A22, presenilin-like aspartic peptidase | 0.0248 | 0.4179 | 1 |
Echinococcus multilocularis | Kelch repeat type 1 | 0.049 | 0.8279 | 0.8279 |
Trypanosoma brucei | Aph-1 protein, putative | 0.0231 | 0.3881 | 0.9136 |
Brugia malayi | hypothetical protein | 0.0121 | 0.2024 | 0.2024 |
Brugia malayi | Presenilin spe-4 | 0.0087 | 0.1447 | 0.1447 |
Schistosoma mansoni | transcription factor LCR-F1 | 0.0186 | 0.3129 | 0.3129 |
Trichomonas vaginalis | Clan AD, family A22, presenilin-like aspartic peptidase | 0.0248 | 0.4179 | 1 |
Entamoeba histolytica | presenilin 1 peptidase, putative | 0.0248 | 0.4179 | 1 |
Echinococcus multilocularis | Nicastrin | 0.0121 | 0.2024 | 0.2024 |
Trypanosoma cruzi | presenilin-like aspartic peptidase, putative | 0.0248 | 0.4179 | 1 |
Echinococcus granulosus | Nicastrin | 0.0121 | 0.2024 | 0.2024 |
Brugia malayi | hypothetical protein | 0.0087 | 0.1447 | 0.1447 |
Echinococcus granulosus | kelch ECH associated protein 1 like | 0.0489 | 0.8256 | 0.8256 |
Loa Loa (eye worm) | gamma-secretase subunit aph-1 | 0.0592 | 1 | 1 |
Echinococcus multilocularis | nicalin | 0.0044 | 0.0728 | 0.0728 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription | 0.0186 | 0.3129 | 0.3129 |
Trypanosoma brucei | presenilin-like aspartic peptidase, putative | 0.0248 | 0.4179 | 1 |
Brugia malayi | hypothetical protein | 0.0087 | 0.1447 | 0.1447 |
Trypanosoma brucei | Presenilin enhancer-2 subunit of gamma secretase, putative | 0.007 | 0.1162 | 0.1259 |
Echinococcus granulosus | gamma secretase subunit aph 1 | 0.0592 | 1 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0186 | 0.3129 | 0.3129 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 696 nM | Modulation of gamma-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in amyloid beta 42 level after overnight incubation by sandwich immunoassay | ChEMBL. | 22650177 |
Inhibition (binding) | Inhibition of gamma-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in total amyloid beta level up to 10 uM after overnight incubation by sandwich immunoassay | ChEMBL. | 22650177 | |
Inhibition (binding) | Inhibition of beta-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in total amyloid beta level up to 10 uM after overnight incubation by sandwich immunoassay | ChEMBL. | 22650177 | |
Inhibition (functional) | = 15 % | Antialzheimer activity in CD1 mouse assessed as reduction in amyloid beta 42 level in brain at 30 mg/kg, po at 4 hrs by ELISA relative to control | ChEMBL. | 22650177 |
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.