Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | thyroid hormone receptor, alpha | Starlite/ChEMBL | References |
Homo sapiens | thyroid hormone receptor, beta | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | photoreceptor-specific nuclear receptor | thyroid hormone receptor, alpha | 451 aa | 372 aa | 25.3 % |
Brugia malayi | photoreceptor-specific nuclear receptor | thyroid hormone receptor, beta | 461 aa | 414 aa | 24.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | nuclear hormone receptor-like 1 | 0.0301 | 0.9282 | 1 |
Schistosoma mansoni | thyroid hormone receptor | 0.0176 | 0.1523 | 1 |
Echinococcus granulosus | Mitotic checkpoint protein PRCC C terminal | 0.0152 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0176 | 0.1523 | 1 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0176 | 0.1523 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (ADMET) | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on heart size at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (functional) | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in liver size at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (ADMET) | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on kidney size at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (functional) | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as lowering glucose level to near normal level | ChEMBL. | 24712661 | |
Activity (functional) | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in cholesterol level at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (functional) | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in liver triglycerides at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (functional) | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as improvement of insulin sensitivity | ChEMBL. | 24712661 | |
Activity (ADMET) | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on bone mineral density at 0.3 to 10 mg/kg, po administered daily for 23 days | ChEMBL. | 24712661 | |
Activity (binding) | = 48.6 % | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T3 | ChEMBL. | 24712661 |
Activity (binding) | = 83.8 % | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T3 | ChEMBL. | 24712661 |
EC50 (binding) | = 0.21 uM | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | ChEMBL. | 24712661 |
EC50 (binding) | = 3.74 uM | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | ChEMBL. | 24712661 |
Fu (ADMET) | = 0.6 % | Fraction unbound in human | ChEMBL. | 24712661 |
IC20 (binding) | = 30 uM | Inhibition of human ERG | ChEMBL. | 24712661 |
IC50 (ADMET) | = 22 uM | Inhibition of CYP2C9 (unknown origin) | ChEMBL. | 24712661 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP3A4 (unknown origin) | ChEMBL. | 24712661 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP3A5 (unknown origin) | ChEMBL. | 24712661 |
IC50 (ADMET) | > 50 uM | Inhibition of CYP2C19 (unknown origin) | ChEMBL. | 24712661 |
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.