Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cholinergic receptor, muscarinic 1 | Starlite/ChEMBL | No references |
Homo sapiens | cholinergic receptor, muscarinic 2 | Starlite/ChEMBL | No references |
Rattus norvegicus | Muscarinic acetylcholine receptor | Starlite/ChEMBL | No references |
Homo sapiens | cholinergic receptor, muscarinic 3 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_133264 | All targets in OG5_133264 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_133264 | All targets in OG5_133264 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | hydroxymethylglutaryl-CoA reductase (NADPH) | 0.1013 | 1 | 0.5 |
Trypanosoma cruzi | 3-hydroxy-3-methylglutaryl-CoA reductase, putative | 0.1013 | 1 | 0.5 |
Mycobacterium ulcerans | hydroxymethylglutaryl-coenzyme a (HMG-CoA) reductase | 0.1013 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.1013 | 1 | 1 |
Echinococcus granulosus | hydroxymethylglutaryl coenzyme A reductase | 0.1013 | 1 | 0.5 |
Echinococcus multilocularis | hydroxymethylglutaryl coenzyme A reductase | 0.1013 | 1 | 0.5 |
Trypanosoma cruzi | 3-hydroxy-3-methylglutaryl-CoA reductase | 0.1013 | 1 | 0.5 |
Trypanosoma brucei | 3-hydroxy-3-methylglutaryl-CoA reductase, putative | 0.1013 | 1 | 0.5 |
Leishmania major | 3-hydroxy-3-methylglutaryl-CoA reductase | 0.1013 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CCh (functional) | = 56 % | Evaluated for its MIPA (muscarinic-stimulated inositol phosphate accumulation) activity measured in SK-N-SH neuroblastoma cells expressing human muscarinic m3 receptor,compound run at 100 microM;100 microM of carbachol was used | ChEMBL. | No reference |
CCh (functional) | = 56 % | Evaluated for its MIPA (muscarinic-stimulated inositol phosphate accumulation) activity measured in SK-N-SH neuroblastoma cells expressing human muscarinic m3 receptor,compound run at 100 microM;100 microM of carbachol was used | ChEMBL. | No reference |
CCh (functional) | = 72 % | Evaluated for its HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1 compound run at 100 microM. | ChEMBL. | No reference |
CCh (functional) | = 72 % | Evaluated for its HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1 compound run at 100 microM. | ChEMBL. | No reference |
EC50 (functional) | = 5.9 uM | Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1 | ChEMBL. | No reference |
EC50 (functional) | = 5.9 uM | Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1 | ChEMBL. | No reference |
EC50 (functional) | = 9.6 uM | Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor | ChEMBL. | No reference |
EC50 (functional) | = 9.6 uM | Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor | ChEMBL. | No reference |
IC50 (binding) | = 3.6 nM | Compound was evaluated for inhibition of [3H]-cis-methyldioxolane binding to label agonist sites (RCMD) in rat neocortex | ChEMBL. | No reference |
IC50 (binding) | = 3.6 nM | Compound was evaluated for inhibition of [3H]-cis-methyldioxolane binding to label agonist sites (RCMD) in rat neocortex | ChEMBL. | No reference |
IC50 (binding) | = 5976 nM | Compound was evaluated for its inhibition of [3H]-quinuclidinyl benzilate binding to label antagonist site (RQNB) in rat neocortex | ChEMBL. | No reference |
IC50 (functional) | = 4.9 uM | Inhibitory activity against human Muscarinic acetylcholine receptor M1 using [3H]-quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | ChEMBL. | No reference |
IC50 (functional) | = 4.9 uM | Inhibitory activity against human Muscarinic acetylcholine receptor M1 using [3H]-quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | ChEMBL. | No reference |
IC50 (functional) | = 8.6 uM | Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]-quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | ChEMBL. | No reference |
IC50 (functional) | = 8.6 uM | Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]-quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | ChEMBL. | No reference |
Ratio (binding) | = 1.8 | Selectivity ratio for m1 over m2 muscarinic receptors was determined | ChEMBL. | No reference |
Ratio (binding) | = 1660 | Ratio of RQNB to RCMD was determined | ChEMBL. | No reference |
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.