Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Neuronal acetylcholine receptor; alpha4/beta2 | Starlite/ChEMBL | References |
Homo sapiens | cholinergic receptor, nicotinic, alpha 4 (neuronal) | Starlite/ChEMBL | References |
Homo sapiens | cholinergic receptor, nicotinic, beta 4 (neuronal) | References | |
Homo sapiens | cholinergic receptor, nicotinic, beta 2 (neuronal) | References | |
Homo sapiens | cholinergic receptor, nicotinic, alpha 7 (neuronal) | Starlite/ChEMBL | References |
Homo sapiens | cholinergic receptor, nicotinic, alpha 3 (neuronal) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | acetylcholine receptor alpha subunit precursor, putative | cholinergic receptor, nicotinic, alpha 7 (neuronal) | 502 aa | 513 aa | 33.9 % |
Brugia malayi | Cation transporter family protein | cholinergic receptor, nicotinic, beta 4 (neuronal) | 498 aa | 508 aa | 31.1 % |
Brugia malayi | Cation transporter family protein | cholinergic receptor, nicotinic, alpha 3 (neuronal) | 505 aa | 486 aa | 34.6 % |
Brugia malayi | Cation transporter family protein | cholinergic receptor, nicotinic, beta 2 (neuronal) | 502 aa | 482 aa | 32.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Loa Loa (eye worm) | hypothetical protein | 0.0183 | 0.1664 | 0.1664 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Onchocerca volvulus | Putative nachr subunit | 0.0269 | 0.4815 | 0.378 |
Echinococcus granulosus | nicotinic acetylcholine receptor alpha subunit | 0.0269 | 0.4815 | 0.988 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0236 | 0.3594 | 0.3594 |
Brugia malayi | nuclear hormone receptor | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | nicotinic acetylcholine receptor alpha subunit | 0.0269 | 0.4815 | 0.4815 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0236 | 0.3594 | 0.2315 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0236 | 0.3594 | 1 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0236 | 0.3594 | 1 |
Brugia malayi | nicotinic acetylcholine receptor alpha subunit, putative | 0.0269 | 0.4815 | 0.378 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0236 | 0.3594 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0236 | 0.3594 | 0.2315 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0236 | 0.3594 | 1 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0398 | 0.9577 | 0.9577 |
Brugia malayi | steroid hormone receptor | 0.0398 | 0.9577 | 0.9492 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | hypothetical protein | 0.0269 | 0.4815 | 0.4815 |
Brugia malayi | nuclear receptor NHR-88 | 0.0236 | 0.3594 | 0.2315 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0236 | 0.3594 | 1 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0236 | 0.3594 | 1 |
Echinococcus multilocularis | nicotinic acetylcholine receptor subunit alpha 8 | 0.0269 | 0.4815 | 1 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0236 | 0.3594 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0236 | 0.3594 | 0.3594 |
Schistosoma mansoni | thyroid hormone receptor | 0.0236 | 0.3594 | 1 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0236 | 0.3594 | 0.2315 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0236 | 0.3594 | 0.2315 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0236 | 0.3594 | 0.3594 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0236 | 0.3594 | 0.3594 |
Echinococcus granulosus | nicotinic acetylcholine receptor subunit alpha 8 | 0.0269 | 0.4815 | 0.988 |
Loa Loa (eye worm) | hypothetical protein | 0.0183 | 0.1664 | 0.1664 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0236 | 0.3594 | 0.2315 |
Schistosoma mansoni | nuclear hormone receptor | 0.0236 | 0.3594 | 1 |
Echinococcus granulosus | nicotinic acetylcholine receptor a11 subunit | 0.0269 | 0.4815 | 0.988 |
Loa Loa (eye worm) | hypothetical protein | 0.0409 | 1 | 1 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0236 | 0.3594 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0236 | 0.3594 | 0.2315 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0236 | 0.3594 | 0.2315 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0236 | 0.3594 | 0.2315 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0236 | 0.3594 | 0.2315 |
Schistosoma mansoni | coup transcription factor | 0.0236 | 0.3594 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0236 | 0.3594 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0236 | 0.3594 | 0.3594 |
Echinococcus multilocularis | nicotinic acetylcholine receptor a11 subunit | 0.0269 | 0.4815 | 1 |
Echinococcus multilocularis | nicotinic acetylcholine receptor alpha subunit | 0.0269 | 0.4815 | 1 |
Echinococcus granulosus | thyroid hormone receptor alpha | 0.0269 | 0.4829 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Schistosoma mansoni | thyroid hormone receptor | 0.0236 | 0.3594 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0236 | 0.3594 | 0.2315 |
Onchocerca volvulus | 0.0236 | 0.3594 | 0.2315 | |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0236 | 0.3594 | 0.3594 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0236 | 0.3594 | 0.3594 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0409 | 1 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0236 | 0.3594 | 0.2315 |
Loa Loa (eye worm) | hypothetical protein | 0.0236 | 0.3594 | 0.3594 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0236 | 0.3594 | 0.2315 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0236 | 0.3594 | 0.2315 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 22 uM | Agonist activity at human alpha3beta4 nAChR expressed in CHO cells assessed as calcium flux by calcium4-based FLIPR assay | ChEMBL. | 22793665 |
EC50 (functional) | = 100 uM | Agonist activity at alpha4beta2 nAChR in human SH-EP1 cells assessed as calcium flux by calcium4-based FLIPR assay | ChEMBL. | 22793665 |
Emax (functional) | = 76 % | Agonist activity at alpha4beta2 nAChR in human SH-EP1 cells assessed as calcium flux by calcium4-based FLIPR assay relative to nicotine | ChEMBL. | 22793665 |
Emax (functional) | = 96 % | Agonist activity at human alpha3beta4 nAChR expressed in CHO cells assessed as calcium flux by calcium4-based FLIPR assay relative to nicotine | ChEMBL. | 22793665 |
Ki (binding) | = 13 nM | Displacement of [3H]nicotine from alpha4beta2 nAChR in human SH-EP1 cells after 2 hrs by liquid scintillation assay | ChEMBL. | 22793665 |
Ki (binding) | = 68 nM | Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat cortex after 2 hrs by liquid scintillation counting | ChEMBL. | 22793665 |
Ki (binding) | = 3.2 uM | Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in CHO cells after 2 hrs by liquid scintillation counting | ChEMBL. | 22793665 |
Ki (binding) | = 8.8 uM | Displacement of [3H]epibatidine from human alpha7 nAChR expressed in CHO cells after 2 hrs by liquid scintillation counting | ChEMBL. | 22793665 |
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.