Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | References | |
Homo sapiens | nuclear receptor subfamily 3, group C, member 2 | References | |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | References | |
Homo sapiens | nuclear receptor subfamily 1, group I, member 2 | References | |
Homo sapiens | RAR-related orphan receptor A | References | |
Homo sapiens | retinoid X receptor, beta | References | |
Homo sapiens | cytochrome P450, family 2, subfamily C, polypeptide 9 | References | |
Homo sapiens | retinoid X receptor, gamma | References | |
Homo sapiens | retinoid X receptor, alpha | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
Mycobacterium tuberculosis | Probable cytochrome P450 136 Cyp136 | cytochrome P450, family 2, subfamily C, polypeptide 9 | 490 aa | 441 aa | 21.8 % |
Brugia malayi | ecdysteroid receptor | retinoid X receptor, gamma | 340 aa | 338 aa | 24.6 % |
Brugia malayi | ecdysteroid receptor | nuclear receptor subfamily 1, group I, member 2 | 434 aa | 427 aa | 25.1 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Nuclear hormone receptor-like 1 | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.008 | 0.0996 | 1 |
Brugia malayi | ecdysteroid receptor | 0.008 | 0.0996 | 1 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.008 | 0.0996 | 1 |
Brugia malayi | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Onchocerca volvulus | 0.008 | 0.0996 | 1 | |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor E75 | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.008 | 0.0996 | 0.0967 |
Brugia malayi | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.008 | 0.0996 | 0.1071 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0047 | 0.0313 | 0.314 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.008 | 0.0996 | 1 |
Brugia malayi | conserved hypotetical protein | 0.0033 | 0.0031 | 0.0314 |
Echinococcus multilocularis | nuclear receptor subfamily 1 group D | 0.0047 | 0.0313 | 0.0313 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0047 | 0.0313 | 0.314 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.008 | 0.0996 | 0.1071 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Brugia malayi | tailless protein | 0.0033 | 0.0031 | 0.0314 |
Echinococcus multilocularis | FTZ F1 alpha | 0.008 | 0.0996 | 0.1071 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.008 | 0.0996 | 0.0967 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.008 | 0.0996 | 0.1071 |
Brugia malayi | steroid hormone receptor | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | ecdysone-induced protein 78c (dr-78) | 0.0047 | 0.0313 | 0.0282 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.008 | 0.0996 | 1 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | Nuclear hormone receptor E75 | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | DR-78 | 0.0033 | 0.0031 | 0.0314 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Brugia malayi | nuclear receptor RXR | 0.0047 | 0.0313 | 0.314 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | nuclear hormone receptor | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.008 | 0.0996 | 0.1071 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0047 | 0.0313 | 0.0282 |
Schistosoma mansoni | nuclear hormone receptor | 0.008 | 0.0996 | 0.0967 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.008 | 0.0996 | 1 |
Echinococcus granulosus | nuclear receptor subfamily 1 group D | 0.0047 | 0.0313 | 0.0282 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.008 | 0.0996 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear receptor NHR-67 | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | nuclear receptor subfamily 1, group D, member 1, putative | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.008 | 0.0996 | 1 |
Brugia malayi | nuclear receptor NHR-67 | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.008 | 0.0996 | 0.0967 |
Brugia malayi | nuclear hormone receptor | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0516 | 1 | 1 |
Brugia malayi | nuclear receptor NHR-88 | 0.0033 | 0.0031 | 0.0314 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.008 | 0.0996 | 0.0967 |
Brugia malayi | nuclear hormone receptor family member odr-7 | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | orphan nuclear receptor NR2E1 | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor | 0.0033 | 0.0031 | 0.0314 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.008 | 0.0996 | 0.1071 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Schistosoma mansoni | coup transcription factor | 0.008 | 0.0996 | 0.0967 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.008 | 0.0996 | 1 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.008 | 0.0996 | 1 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.008 | 0.0996 | 0.0967 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.008 | 0.0996 | 0.1071 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.008 | 0.0996 | 0.0967 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.008 | 0.0996 | 0.0967 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.047 | 0.9036 | 1 |
Brugia malayi | ecdysone receptor | 0.0033 | 0.0031 | 0.0314 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.008 | 0.0996 | 0.1071 |
Brugia malayi | nuclear hormone receptor family member nhr-6 | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Schistosoma mansoni | thyroid hormone receptor | 0.008 | 0.0996 | 0.0967 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.008 | 0.0996 | 1 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.008 | 0.0996 | 0.1071 |
Loa Loa (eye worm) | steroid hormone receptor | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0033 | 0.0031 | 0.0314 |
Echinococcus granulosus | FTZ F1 alpha | 0.008 | 0.0996 | 0.0967 |
Onchocerca volvulus | Bile acid receptor homolog | 0.008 | 0.0996 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor-like 1 | 0.0047 | 0.0313 | 0.314 |
Brugia malayi | nuclear receptor NHR-88 | 0.008 | 0.0996 | 1 |
Brugia malayi | hypothetical protein | 0.0047 | 0.0313 | 0.314 |
Brugia malayi | nuclear receptor RXR | 0.0033 | 0.0031 | 0.0314 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.008 | 0.0996 | 1 |
Schistosoma mansoni | thyroid hormone receptor | 0.008 | 0.0996 | 0.0967 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 | |
Activity (binding) | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 | |
EC50 (binding) | = 4 nM | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 |
EC50 (binding) | = 6 nM | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 |
EC50 (binding) | = 21 nM | Agonist activity at human LXRbeta ligand binding domain(155 to 460 residues) transfected in HEK293 cells after 16 hrs by Gal4-luciferase reporter gene assay | ChEMBL. | 26990539 |
EC50 (binding) | = 21 nM | Agonist activity at LXRbeta LBD (unknown origin) fused with Gal4-DNA binding domain expressed in HEK293 cells assessed as modulation of receptor transcription activity by luciferase reporter gene assay | LITERATURE. | 27599745 |
Efficacy (binding) | = 56 % | Agonist activity at LXRbeta LBD (unknown origin) fused with Gal4-DNA binding domain expressed in HEK293 cells assessed as modulation of receptor transcription activity by luciferase reporter gene assay relative to T0901317 | LITERATURE. | 27599745 |
Efficacy (binding) | = 56 % | Agonist activity at human LXRbeta ligand binding domain(155 to 460 residues) transfected in HEK293 cells after 16 hrs by Gal4-luciferase reporter gene assay relative to TO901317 | ChEMBL. | 26990539 |
Efficacy (binding) | = 91 % | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 |
Efficacy (binding) | = 101 % | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression after 24 hrs by RT-PCR analysis | ChEMBL. | 26990539 |
FC (binding) | = 1.32 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 1 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 1.62 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 1 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 1.87 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 2 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 2.43 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 2 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 2.67 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 6 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 2.86 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 5 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 3.05 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 19 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 3.5 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 56 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 3.72 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 16 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 3.78 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 167 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 4.3 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 50 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 4.47 | Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 500 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 4.87 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 158 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
FC (binding) | = 5.45 | Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 500 nM after 24 hrs by RT-PCR analysis relative to control | ChEMBL. | 26990539 |
IC50 (ADMET) | Inhibition of CYP2D6 in human liver microsomes | ChEMBL. | 26990539 | |
IC50 (ADMET) | = 608 nM | Inhibition of CYP2C9 (unknown origin) | LITERATURE. | 27599745 |
IC50 (ADMET) | = 610 nM | Inhibition of recombinant CYP2C9 (unknown origin) | ChEMBL. | 26990539 |
IC50 (ADMET) | = 2200 nM | Inhibition of CYP2C9 in human liver microsomes | ChEMBL. | 26990539 |
IC50 (ADMET) | = 6600 nM | Inhibition of CYP3A4 in human liver microsomes | ChEMBL. | 26990539 |
IC50 (binding) | > 10000 nM | Inhibition of RXR (unknown origin) | ChEMBL. | 26990539 |
IC50 (binding) | > 10000 nM | Inhibition of Mineralocorticoid receptor (unknown origin) | ChEMBL. | 26990539 |
IC50 (binding) | > 10000 nM | Inhibition of PXR (unknown origin) | ChEMBL. | 26990539 |
IC50 (binding) | > 10000 nM | Inhibition of RORalpha receptor (unknown origin) | ChEMBL. | 26990539 |
IC50 (ADMET) | = 29430 nM | Inhibition of recombinant CYP3A4 (unknown origin) | ChEMBL. | 26990539 |
IC50 (ADMET) | = 29450 nM | Inhibition of CYP3A4 (unknown origin) | LITERATURE. | 27599745 |
IC50 (ADMET) | > 30000 nM | Inhibition of CYP2D6 (unknown origin) | LITERATURE. | 27599745 |
IC50 (ADMET) | > 30000 nM | Inhibition of recombinant CYP2D6 (unknown origin) | ChEMBL. | 26990539 |
Ki (binding) | = 3 nM | Displacement of [3H]TO901317 from LXRbeta ligand binding domain (unknown origin) after 30 mins by liquid scintillation counting | ChEMBL. | 26990539 |
Ki (binding) | = 3 nM | Displacement of radiolabeled T0901317 from LXRbeta LBD (unknown origin) | LITERATURE. | 27599745 |
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.
2 literature references were collected for this gene.