Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Oryctolagus cuniculus | Acyl-CoA:cholesterol acyltransferase | Starlite/ChEMBL | No references |
Homo sapiens | sterol O-acyltransferase 1 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
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 |
Schistosoma mansoni | sterol O-acyltransferase 1 | Get druggable targets OG5_133487 | All targets in OG5_133487 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Toxoplasma gondii | acyl-CoA:cholesterol acyltransferase alpha ACAT1-alpha | sterol O-acyltransferase 1 | 492 aa | 413 aa | 25.9 % |
Dictyostelium discoideum | diacylglycerol O-acyltransferase 1 | Acyl-CoA:cholesterol acyltransferase | 305 aa | 278 aa | 21.9 % |
Neospora caninum | sterol O-acyltransferase, putative | Acyl-CoA:cholesterol acyltransferase | 305 aa | 258 aa | 20.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | sterol O acyltransferase 1 | 0.0528 | 1 | 1 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus granulosus | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Loa Loa (eye worm) | hypothetical protein | 0.0105 | 0.0376 | 0.0376 |
Loa Loa (eye worm) | hypothetical protein | 0.0528 | 1 | 1 |
Loa Loa (eye worm) | thrombospondin type 1 domain-containing protein | 0.0227 | 0.315 | 0.315 |
Brugia malayi | Thrombospondin type 1 domain containing protein | 0.0227 | 0.315 | 1 |
Echinococcus granulosus | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Loa Loa (eye worm) | hypothetical protein | 0.0105 | 0.0376 | 0.0376 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus granulosus | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus multilocularis | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus granulosus | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Echinococcus granulosus | ectonucleotide pyrophosphatase:phosphodiesterase | 0.0105 | 0.0376 | 0.0376 |
Onchocerca volvulus | 0.0227 | 0.315 | 1 | |
Loa Loa (eye worm) | hypothetical protein | 0.0476 | 0.8826 | 0.8826 |
Schistosoma mansoni | sterol O-acyltransferase 1 | 0.0528 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0105 | 0.0376 | 0.0376 |
Schistosoma mansoni | hypothetical protein | 0.0227 | 0.315 | 0.2882 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | = 286 | Inhibition of microsomal acylcoA: cholesterol acyltransferase in the presence of plasma from rats administered orally with 100 mg/kg of the compound; pmoles [14C]-Cholesteryl oleate formed / mg protein / min incubation | ChEMBL. | No reference |
Activity (binding) | = 286 | Inhibition of microsomal acylcoA: cholesterol acyltransferase in the presence of plasma from rats administered orally with 100 mg/kg of the compound; pmoles [14C]-Cholesteryl oleate formed / mg protein / min incubation | ChEMBL. | No reference |
IC50 (binding) | = 24.2 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from cholesterol-fed rabbit thoracic aorta | ChEMBL. | No reference |
IC50 (binding) | = 24.2 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from cholesterol-fed rabbit thoracic aorta | ChEMBL. | No reference |
IC50 (binding) | = 27 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from cholesterol-fed rabbit intestinal mucosa | ChEMBL. | No reference |
IC50 (binding) | = 27 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from cholesterol-fed rabbit intestinal mucosa | ChEMBL. | No reference |
IC50 (binding) | = 63 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from monkey liver | ChEMBL. | No reference |
IC50 (binding) | = 63 nM | Inhibitory activity against acylcoA: cholesterol acyltransferase (ACAT) in microsomes from monkey liver | ChEMBL. | No reference |
Plasma lipids (functional) | = 18 mg dl-1 | Effect of single oral administration of 15 mg/kg of compound on free cholesterol of hypercholesterolemic rats | ChEMBL. | No reference |
Plasma lipids (functional) | = 57 mg dl-1 | Effect of single oral administration of 15 mg/kg of compound on cholesterol esters of hypercholesterolemic rats | ChEMBL. | No reference |
Plasma lipids (functional) | = 76 mg dl-1 | Effect of single oral administration of 15 mg/kg of compound on triglycerides of hypercholesterolemic rats | ChEMBL. | No reference |
Plasma lipids (functional) | = 77 mg dl-1 | Effect of single oral administration of 15 mg/kg of compound on phospholipids of hypercholesterolemic rats | ChEMBL. | No reference |
Ratio (functional) | = 0.27 | Ratio of effect of single oral administration of 15 mg/kg of compound on liver free cholesterol/cholesterol esters of hypercholesterolemic rats | ChEMBL. | No reference |
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.