Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Muscarinic acetylcholine receptor M1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus multilocularis | serotonin receptor | Muscarinic acetylcholine receptor M1 | 460 aa | 432 aa | 26.6 % |
Loa Loa (eye worm) | hypothetical protein | Muscarinic acetylcholine receptor M1 | 460 aa | 425 aa | 22.1 % |
Schistosoma japonicum | ko:K04136 adrenergic receptor, alpha 1b, putative | Muscarinic acetylcholine receptor M1 | 460 aa | 462 aa | 23.4 % |
Schistosoma mansoni | amine GPCR | Muscarinic acetylcholine receptor M1 | 460 aa | 463 aa | 27.0 % |
Echinococcus granulosus | biogenic amine 5HT receptor | Muscarinic acetylcholine receptor M1 | 460 aa | 432 aa | 26.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Chlamydia trachomatis | dihydrofolate reductase | 0.2255 | 1 | 0.5 |
Loa Loa (eye worm) | thymidylate synthase | 0.0184 | 0.0484 | 0.0484 |
Echinococcus multilocularis | thymidylate synthase | 0.0184 | 0.0484 | 0.0484 |
Echinococcus granulosus | thymidylate synthase | 0.0184 | 0.0484 | 0.0484 |
Onchocerca volvulus | 0.0184 | 0.0484 | 1 | |
Mycobacterium tuberculosis | Probable thymidylate synthase ThyA (ts) (TSASE) | 0.0184 | 0.0484 | 0.0446 |
Schistosoma mansoni | lipoxygenase | 0.0118 | 0.018 | 0.018 |
Echinococcus granulosus | dihydrofolate reductase | 0.2255 | 1 | 1 |
Loa Loa (eye worm) | dihydrofolate reductase | 0.2255 | 1 | 1 |
Echinococcus multilocularis | dihydrofolate reductase | 0.2255 | 1 | 1 |
Mycobacterium ulcerans | dihydrofolate reductase DfrA | 0.2255 | 1 | 1 |
Trypanosoma cruzi | dihydrofolate reductase-thymidylate synthase | 0.1046 | 0.4446 | 1 |
Mycobacterium tuberculosis | Dihydrofolate reductase DfrA (DHFR) (tetrahydrofolate dehydrogenase) | 0.2255 | 1 | 1 |
Schistosoma mansoni | dihydrofolate reductase | 0.2255 | 1 | 1 |
Brugia malayi | thymidylate synthase | 0.0184 | 0.0484 | 0.0484 |
Mycobacterium leprae | DIHYDROFOLATE REDUCTASE DFRA (DHFR) (TETRAHYDROFOLATE DEHYDROGENASE) | 0.2255 | 1 | 1 |
Brugia malayi | hypothetical protein | 0.0088 | 0.004 | 0.004 |
Schistosoma mansoni | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0184 | 0.0484 | 0.0484 |
Trypanosoma brucei | dihydrofolate reductase-thymidylate synthase | 0.1046 | 0.4446 | 0.5 |
Leishmania major | dihydrofolate reductase-thymidylate synthase | 0.1046 | 0.4446 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0088 | 0.004 | 0.5 |
Echinococcus granulosus | arachidonate 5 lipoxygenase | 0.0118 | 0.018 | 0.018 |
Toxoplasma gondii | bifunctional dihydrofolate reductase-thymidylate synthase | 0.1046 | 0.4446 | 0.5 |
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | 0.1046 | 0.4446 | 0.5 |
Brugia malayi | Dihydrofolate reductase | 0.2255 | 1 | 1 |
Schistosoma mansoni | lipoxygenase | 0.0083 | 0.0017 | 0.0017 |
Plasmodium vivax | bifunctional dihydrofolate reductase-thymidylate synthase, putative | 0.1046 | 0.4446 | 0.5 |
Echinococcus multilocularis | arachidonate 5 lipoxygenase | 0.0118 | 0.018 | 0.018 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 0.36 mM | Tested for stimulating PI(phosphoinositol) hydrolysis in A9L-m1 cells, activity expressed as EC50 mM. | ChEMBL. | 7658434 |
EC50 (functional) | = 0.52 mM | Tested for stimulating PI(phosphoinositol) hydrolysis in A9L-m1 cells, activity expressed as EC50 mM. | ChEMBL. | 7658434 |
EC50 (functional) | = 0.52 mM | Tested for stimulating PI(phosphoinositol) hydrolysis in A9L-m1 cells, activity expressed as EC50 mM. | ChEMBL. | 7658434 |
EC50 (functional) | = 1.73 mM | Tested for stimulating PI(phosphoinositol) hydrolysis in A9L-m1 cells, activity expressed as EC50 mM. | ChEMBL. | 7658434 |
IC50 (binding) | = 2.5 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-OXO-M as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 3.7 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 4.5 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-OXO-M as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 4.5 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-OXO-M as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 6 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 6 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 10.6 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | ChEMBL. | 7658434 |
IC50 (binding) | = 11.3 nM | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-OXO-M as the radioligand. | ChEMBL. | 7658434 |
Max (functional) | = 33 % | Stimulating PI (phosphoinositol) hydrolysis in A9L-m1 cells. | ChEMBL. | 7658434 |
Max (functional) | = 40 % | Stimulating PI (phosphoinositol) hydrolysis in A9L-m1 cells. | ChEMBL. | 7658434 |
Max (functional) | = 40 % | Stimulating PI (phosphoinositol) hydrolysis in A9L-m1 cells. | ChEMBL. | 7658434 |
Max (functional) | = 46 % | Stimulating PI (phosphoinositol) hydrolysis in A9L-m1 cells. | ChEMBL. | 7658434 |
Score (functional) | = 0 | Effect on salivation in mice, after intraperitoneal administration of 10mg/kg, activity expressed as a score using a scale of 0-2. | ChEMBL. | 7658434 |
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.