Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 3 | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Brugia malayi | ecdysteroid receptor | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Onchocerca volvulus | Bile acid receptor homolog | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | photoreceptor-specific nuclear receptor | nuclear receptor subfamily 1, group H, member 3 | 387 aa | 321 aa | 28.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0207 | 1 | 1 |
Echinococcus multilocularis | jun protein | 0.0084 | 0.2237 | 0.4167 |
Echinococcus granulosus | Transcription factor JmjC domain containing protein | 0.0059 | 0.0691 | 0.1288 |
Loa Loa (eye worm) | hypothetical protein | 0.005 | 0.0099 | 0.0099 |
Schistosoma mansoni | hypothetical protein | 0.0134 | 0.5396 | 0.7627 |
Loa Loa (eye worm) | hypothetical protein | 0.0081 | 0.2093 | 0.2093 |
Schistosoma mansoni | soluble guanylate cyclase gcy | 0.0141 | 0.5868 | 0.8293 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0133 | 0.5369 | 0.7589 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0207 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0161 | 0.7075 | 0.7075 |
Loa Loa (eye worm) | jmjC domain-containing protein | 0.0059 | 0.0691 | 0.0691 |
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.005 | 0.0099 | 0.0099 |
Brugia malayi | Adenylate and Guanylate cyclase catalytic domain containing protein | 0.0161 | 0.7075 | 0.7075 |
Loa Loa (eye worm) | carboxylesterase | 0.0133 | 0.5369 | 0.5369 |
Schistosoma mansoni | jun-related protein | 0.0068 | 0.1252 | 0.1769 |
Schistosoma mansoni | soluble guanylate cyclase gcy | 0.0161 | 0.7075 | 1 |
Schistosoma mansoni | lipoxygenase | 0.0118 | 0.4428 | 0.6259 |
Brugia malayi | jmjC domain containing protein | 0.0059 | 0.0691 | 0.0691 |
Schistosoma mansoni | lipoxygenase | 0.0083 | 0.2185 | 0.3089 |
Schistosoma mansoni | hypothetical protein | 0.0068 | 0.1252 | 0.1769 |
Echinococcus multilocularis | acetylcholinesterase | 0.0133 | 0.5369 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0052 | 0.0243 | 0.0344 |
Echinococcus multilocularis | arachidonate 5 lipoxygenase | 0.0118 | 0.4428 | 0.8247 |
Schistosoma mansoni | jumonji/arid domain-containing protein | 0.0059 | 0.0691 | 0.0977 |
Onchocerca volvulus | 0.0161 | 0.7075 | 0.6711 | |
Brugia malayi | Carboxylesterase family protein | 0.0133 | 0.5369 | 0.5369 |
Echinococcus granulosus | acetylcholinesterase | 0.0133 | 0.5369 | 1 |
Loa Loa (eye worm) | guanylyl cyclase/natriuretic peptide receptor | 0.0161 | 0.7075 | 0.7075 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.005 | 0.0099 | 0.0099 |
Echinococcus granulosus | jun protein | 0.0084 | 0.2237 | 0.4167 |
Brugia malayi | Carboxylesterase family protein | 0.0133 | 0.5369 | 0.5369 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription factor | 0.0084 | 0.2237 | 0.4167 |
Schistosoma mansoni | jumonji/arid domain-containing protein | 0.0059 | 0.0691 | 0.0977 |
Loa Loa (eye worm) | hypothetical protein | 0.0133 | 0.5369 | 0.5369 |
Echinococcus granulosus | carboxylesterase 5A | 0.0133 | 0.5369 | 1 |
Schistosoma mansoni | soluble guanylate cyclase gcy | 0.0141 | 0.5868 | 0.8293 |
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.005 | 0.0099 | 0.0099 |
Echinococcus granulosus | acetylcholinesterase | 0.0133 | 0.5369 | 1 |
Schistosoma mansoni | jumonji domain containing protein | 0.0059 | 0.0691 | 0.0977 |
Echinococcus multilocularis | Transcription factor, JmjC domain containing protein | 0.0059 | 0.0691 | 0.1288 |
Loa Loa (eye worm) | hypothetical protein | 0.0133 | 0.5369 | 0.5369 |
Schistosoma mansoni | soluble guanylyl cyclase beta-3 | 0.0134 | 0.5396 | 0.7627 |
Brugia malayi | bZIP transcription factor family protein | 0.0084 | 0.2237 | 0.2237 |
Echinococcus multilocularis | acetylcholinesterase | 0.0133 | 0.5369 | 1 |
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.0133 | 0.5369 | 0.5369 |
Schistosoma mansoni | soluble guanylate cyclase gcy | 0.0141 | 0.5868 | 0.8293 |
Echinococcus multilocularis | lysine specific demethylase 5A | 0.0059 | 0.0691 | 0.1288 |
Brugia malayi | jmjC domain containing protein | 0.0059 | 0.0691 | 0.0691 |
Brugia malayi | hypothetical protein | 0.0066 | 0.1107 | 0.1107 |
Echinococcus granulosus | lysine specific demethylase 5A | 0.0059 | 0.0691 | 0.1288 |
Echinococcus multilocularis | carboxylesterase 5A | 0.0133 | 0.5369 | 1 |
Echinococcus granulosus | arachidonate 5 lipoxygenase | 0.0118 | 0.4428 | 0.8247 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription factor | 0.0084 | 0.2237 | 0.4167 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Transactivation of PXR by luciferase reporter gene assay | ChEMBL. | 16876993 | |
Activity (functional) | Transactivation of FXR by luciferase reporter gene assay | ChEMBL. | 16876993 | |
Activity (functional) | 0 | Transactivation of PXR by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | 0 | Transactivation of FXR by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | = 11 % | Decrease in plasma triglyceride level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Activity (functional) | = 11 % | Decrease in plasma triglyceride level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Activity (functional) | = 12 % | Increase in plasma HDL-C level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Activity (functional) | = 12 % | Increase in plasma HDL-C level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Activity (functional) | = 81 % | Transactivation of LXRalpha relative to T0901317 by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | = 81 % | Transactivation of LXRalpha relative to T0901317 by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | = 105 % | Transactivation of LXRbeta relative to T0901317 by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | = 105 % | Transactivation of LXRbeta relative to T0901317 by luciferase reporter gene assay | ChEMBL. | 16876993 |
Activity (functional) | = 520 % | Increase in liver triglyceride level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Activity (functional) | = 520 % | Increase in liver triglyceride level in C57BL/6J mouse after 5 days at 100 mg/kg/day relative to control | ChEMBL. | 16876993 |
Cp (ADMET) | = 2300 ng/ml | Plasma concentration in C57BL/6J mouse after 5 days at 100 mg/kg/day | ChEMBL. | 16876993 |
Cp (ADMET) | = 2300 ng/ml | Plasma concentration in C57BL/6J mouse after 5 days at 100 mg/kg/day | ChEMBL. | 16876993 |
Drug uptake (ADMET) | = 6300 ng/g | Liver concentration in C57BL/6J mouse after 5 days at 100 mg/kg/day | ChEMBL. | 16876993 |
Drug uptake (ADMET) | = 6300 ng/g | Liver concentration in C57BL/6J mouse after 5 days at 100 mg/kg/day | ChEMBL. | 16876993 |
EC50 (functional) | = 0.03 uM | Transactivation of LXRbeta by luciferase reporter gene assay | ChEMBL. | 16876993 |
EC50 (functional) | = 0.03 uM | Transactivation of LXRbeta by luciferase reporter gene assay | ChEMBL. | 16876993 |
EC50 (functional) | = 0.1 uM | Transactivation of LXRalpha by luciferase reporter gene assay | ChEMBL. | 16876993 |
EC50 (functional) | = 0.1 uM | Transactivation of LXRalpha by luciferase reporter gene assay | ChEMBL. | 16876993 |
IC50 (binding) | = 0.008 uM | Binding affinity to LXRbeta by radioligand displacement assay | ChEMBL. | 16876993 |
IC50 (binding) | = 0.008 uM | Binding affinity to LXRbeta by radioligand displacement assay | ChEMBL. | 16876993 |
IC50 (binding) | = 0.05 uM | Binding affinity to LXRalpha by radioligand displacement assay | ChEMBL. | 16876993 |
IC50 (binding) | = 0.05 uM | Binding affinity to LXRalpha by radioligand displacement assay | ChEMBL. | 16876993 |
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.