Species | Target name | Source | Bibliographic reference |
---|---|---|---|
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, beta | 461 aa | 414 aa | 24.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0312 | 0.8986 | 0.8986 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0042 | 0.0552 | 0.0552 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0042 | 0.0552 | 0.5 |
Toxoplasma gondii | cell-cycle-associated protein kinase CDK, putative | 0.0042 | 0.0552 | 0.5 |
Echinococcus multilocularis | cyclin dependent kinase | 0.0042 | 0.0552 | 0.0552 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0024 | 0 | 0.5 |
Echinococcus multilocularis | cyclin dependent kinase 1 | 0.0042 | 0.0552 | 0.0552 |
Trypanosoma cruzi | cdc2-related kinase 3 | 0.0042 | 0.0552 | 0.5 |
Echinococcus granulosus | Mitotic checkpoint protein PRCC C terminal | 0.0152 | 0.3983 | 0.3983 |
Schistosoma mansoni | thyroid hormone receptor | 0.0176 | 0.4744 | 0.4744 |
Loa Loa (eye worm) | CMGC/CDK/CDK5 protein kinase | 0.0042 | 0.0552 | 0.0552 |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0042 | 0.0552 | 0.5 |
Trypanosoma cruzi | cdc2-related kinase 1 | 0.0042 | 0.0552 | 0.5 |
Echinococcus granulosus | cyclin dependent kinase 1 | 0.0042 | 0.0552 | 0.0552 |
Giardia lamblia | Kinase, CMGC CDK | 0.0042 | 0.0552 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0024 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0042 | 0.0538 | 0.0538 |
Echinococcus multilocularis | tyrosine protein phosphatase non receptor type | 0.0345 | 1 | 1 |
Onchocerca volvulus | 0.0024 | 0 | 0.5 | |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0042 | 0.0552 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0301 | 0.8626 | 0.8626 |
Plasmodium falciparum | protein kinase 5 | 0.0042 | 0.0552 | 0.5 |
Leishmania major | cell division protein kinase 2,cdc2-related kinase | 0.0042 | 0.0552 | 0.5 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0042 | 0.0552 | 0.0552 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0024 | 0 | 0.5 |
Echinococcus multilocularis | cyclin dependent kinase 1 | 0.0042 | 0.0552 | 0.0552 |
Echinococcus multilocularis | Mitotic checkpoint protein PRCC, C terminal | 0.0152 | 0.3983 | 0.3983 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0042 | 0.0552 | 0.0552 |
Brugia malayi | cell division control protein 2 homolog | 0.0042 | 0.0552 | 0.0552 |
Loa Loa (eye worm) | nuclear hormone receptor-like 1 | 0.0301 | 0.8626 | 0.8626 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0042 | 0.0552 | 0.5 |
Echinococcus granulosus | tyrosine protein phosphatase non receptor type | 0.0345 | 1 | 1 |
Loa Loa (eye worm) | protein-tyrosine phosphatase | 0.0345 | 1 | 1 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0301 | 0.8626 | 0.8626 |
Trypanosoma brucei | cdc2-related kinase 1 | 0.0042 | 0.0552 | 0.5 |
Schistosoma mansoni | protein tyrosine phosphatase non-receptor type nt1 | 0.0345 | 1 | 1 |
Echinococcus multilocularis | cyclin dependent kinase 5 | 0.0042 | 0.0552 | 0.0552 |
Trypanosoma cruzi | cdc2-related kinase 1 | 0.0042 | 0.0552 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0176 | 0.4744 | 0.4744 |
Echinococcus granulosus | 5'partial|cyclin dependent kinase 1 | 0.0042 | 0.0552 | 0.0552 |
Trypanosoma brucei | cdc2-related kinase 3 | 0.0042 | 0.0552 | 0.5 |
Leishmania major | cell division related protein kinase 2,cdc2-related kinase | 0.0042 | 0.0552 | 0.5 |
Trypanosoma cruzi | cdc2-related kinase 3 | 0.0042 | 0.0552 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0299 | 0.8583 | 0.8583 |
Schistosoma mansoni | hypothetical protein | 0.0152 | 0.3983 | 0.3983 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0042 | 0.0552 | 0.0552 |
Echinococcus granulosus | cyclin dependent kinase 5 | 0.0042 | 0.0552 | 0.0552 |
Plasmodium vivax | protein kinase Crk2 | 0.0042 | 0.0552 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0042 | 0.0552 | 0.0552 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0176 | 0.4744 | 0.4744 |
Giardia lamblia | Kinase, CMGC CDK | 0.0042 | 0.0552 | 0.5 |
Echinococcus granulosus | cyclin dependent kinase | 0.0042 | 0.0552 | 0.0552 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0042 | 0.0552 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 15.2 uM | Displacement of labeled SRC2-2 from human TRbeta expressed in BL21 (DE3) cells FP assay | ChEMBL. | 17918822 |
IC50 (binding) | = 15.2 uM | Displacement of labeled SRC2-2 from human TRbeta expressed in BL21 (DE3) cells FP assay | ChEMBL. | 17918822 |
IC50 (binding) | = 25.8 uM | Displacement of labeled SRC2-2 from human TRalpha by FP assay | ChEMBL. | 17918822 |
IC50 (binding) | = 25.8 uM | Displacement of labeled SRC2-2 from human TRalpha by FP assay | ChEMBL. | 17918822 |
LD50 (functional) | = 107 uM | Cytotoxicity against human ARO cells after 48 hrs by MTS assay | ChEMBL. | 17918822 |
LD50 (functional) | = 107 uM | Cytotoxicity against human ARO cells after 48 hrs by MTS assay | ChEMBL. | 17918822 |
LD50 (functional) | = 160 uM | Cytotoxicity against human U2OS cells after 48 hrs by MTS assay | ChEMBL. | 17918822 |
LD50 (functional) | = 160 uM | Cytotoxicity against human U2OS cells after 48 hrs by MTS assay | ChEMBL. | 17918822 |
permeability (ADMET) | = 254 10^-6 cm/s | Permeability across artificial membrane at pH 7.4 by PAMPA assay | ChEMBL. | 17918822 |
Ratio IC50 (binding) | = 1.7 | Selectivity ratio of IC50 for TRBeta to IC50 for TRalpha | ChEMBL. | 17918822 |
Solubility | = 354 uM | Solubility in PBS | ChEMBL. | 17918822 |
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.