Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Oryctolagus cuniculus | Acyl-CoA:cholesterol acyltransferase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Schistosoma mansoni | sterol O-acyltransferase 1 | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Schistosoma japonicum | ko:K00637 sterol O-acyltransferase [EC2.3.1.26], putative | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Echinococcus multilocularis | sterol O acyltransferase 1 | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Echinococcus granulosus | sterol O acyltransferase 1 | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Neospora caninum | sterol O-acyltransferase, putative | Acyl-CoA:cholesterol acyltransferase | 305 aa | 258 aa | 20.2 % |
Dictyostelium discoideum | diacylglycerol O-acyltransferase 1 | Acyl-CoA:cholesterol acyltransferase | 305 aa | 278 aa | 21.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma brucei | dihydrofolate reductase-thymidylate synthase | 0.102 | 0.8978 | 0.5 |
Echinococcus granulosus | thymidylate synthase | 0.0441 | 0.2898 | 0.2898 |
Loa Loa (eye worm) | hypothetical protein | 0.0264 | 0.1043 | 0.0293 |
Echinococcus granulosus | dihydrofolate reductase | 0.1118 | 1 | 1 |
Echinococcus multilocularis | thymidylate synthase | 0.0441 | 0.2898 | 0.2898 |
Mycobacterium ulcerans | dihydrofolate reductase DfrA | 0.1118 | 1 | 1 |
Chlamydia trachomatis | dihydrofolate reductase | 0.1118 | 1 | 0.5 |
Leishmania major | dihydrofolate reductase-thymidylate synthase | 0.102 | 0.8978 | 0.5 |
Mycobacterium leprae | DIHYDROFOLATE REDUCTASE DFRA (DHFR) (TETRAHYDROFOLATE DEHYDROGENASE) | 0.1118 | 1 | 1 |
Brugia malayi | Dihydrofolate reductase | 0.1118 | 1 | 1 |
Echinococcus multilocularis | muscleblind protein | 0.0296 | 0.1375 | 0.1375 |
Loa Loa (eye worm) | hypothetical protein | 0.0296 | 0.1375 | 0.0653 |
Mycobacterium tuberculosis | Probable thymidylate synthase ThyA (ts) (TSASE) | 0.0441 | 0.2898 | 0.2545 |
Toxoplasma gondii | bifunctional dihydrofolate reductase-thymidylate synthase | 0.102 | 0.8978 | 0.5 |
Echinococcus multilocularis | sterol O acyltransferase 1 | 0.0264 | 0.1043 | 0.1043 |
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | 0.102 | 0.8978 | 0.5 |
Echinococcus granulosus | sterol O acyltransferase 1 | 0.0264 | 0.1043 | 0.1043 |
Echinococcus granulosus | muscleblind protein | 0.0296 | 0.1375 | 0.1375 |
Mycobacterium tuberculosis | Dihydrofolate reductase DfrA (DHFR) (tetrahydrofolate dehydrogenase) | 0.1118 | 1 | 1 |
Trypanosoma cruzi | dihydrofolate reductase-thymidylate synthase | 0.102 | 0.8978 | 1 |
Echinococcus multilocularis | muscleblind protein 1 | 0.0296 | 0.1375 | 0.1375 |
Onchocerca volvulus | 0.0441 | 0.2898 | 0.5 | |
Loa Loa (eye worm) | dihydrofolate reductase | 0.1118 | 1 | 1 |
Trichomonas vaginalis | conserved hypothetical protein | 0.021 | 0.0474 | 0.5 |
Schistosoma mansoni | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0441 | 0.2898 | 0.2898 |
Brugia malayi | Muscleblind-like protein | 0.0296 | 0.1375 | 0.0946 |
Schistosoma mansoni | sterol O-acyltransferase 1 | 0.0264 | 0.1043 | 0.1043 |
Brugia malayi | thymidylate synthase | 0.0441 | 0.2898 | 0.2545 |
Loa Loa (eye worm) | thymidylate synthase | 0.0441 | 0.2898 | 0.2304 |
Echinococcus multilocularis | dihydrofolate reductase | 0.1118 | 1 | 1 |
Schistosoma mansoni | dihydrofolate reductase | 0.1118 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0296 | 0.1375 | 0.0653 |
Plasmodium vivax | bifunctional dihydrofolate reductase-thymidylate synthase, putative | 0.102 | 0.8978 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.27 uM | In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase in liver microsomes isolated from cholesterol-fed rabbits | ChEMBL. | 8145231 |
IC50 (binding) | = 0.27 uM | In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase in liver microsomes isolated from cholesterol-fed rabbits | ChEMBL. | 8145231 |
Reduction (functional) | = 49 % | In vivo hypocholesterolemic activity in golden hamsters, fed with a diet containing 2% cholesterol at a dose of 100 mg/kg | ChEMBL. | 8145231 |
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.