Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Cavia porcellus | Muscarinic acetylcholine receptor M3 | Starlite/ChEMBL | References |
Homo sapiens | cholinergic receptor, muscarinic 3 | Starlite/ChEMBL | 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 | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | Glycoprotein hormone beta 5 homolog | Muscarinic acetylcholine receptor M3 | 587 aa | 506 aa | 34.6 % |
Schistosoma mansoni | muscarinic acetylcholine (GAR) receptor | Muscarinic acetylcholine receptor M3 | 587 aa | 504 aa | 26.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.4356 | 1 | 1 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.225 | 0.3714 | 1 |
Leishmania major | choline/Carnitine o-acyltransferase-like protein | 0.225 | 0.3714 | 1 |
Echinococcus granulosus | carnitine O palmitoyltransferase 1 liver | 0.225 | 0.3714 | 1 |
Loa Loa (eye worm) | choline/Carnitine O-acyltransferase | 0.1145 | 0.0416 | 0.0416 |
Trypanosoma brucei | carnitine O-palmitoyltransferase II, putative | 0.1145 | 0.0416 | 0.5 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.225 | 0.3714 | 1 |
Echinococcus multilocularis | carnitine O palmitoyltransferase 1, liver | 0.225 | 0.3714 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CL (ADMET) | = 65 uL/min/10^6cells | Intrinsic clearance in human hepatocytes assessed per million cells | ChEMBL. | 21870878 |
IC50 (functional) | = 4.3 nM | Antagonist activity at M3 receptor in Dunkin-Hartley guinea pig tracheal strips assessed as inhibition of electrically field-stimulated contractile response after 8 hrs | ChEMBL. | 21870878 |
Ki (binding) | = 0.18 nM | Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay | ChEMBL. | 21870878 |
Ki (functional) | = 0.21 nM | Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry | ChEMBL. | 21870878 |
T1/2 (binding) | > 1440 min | Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells assessed as dissociation half life at 100 fold human M1 receptor binding Ki concentration after 2 hrs by dilution-offset filter binding assay | ChEMBL. | 21870878 |
T1/2 (binding) | > 1440 min | Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells assessed as dissociation half life at 100 fold human M1 receptor binding Ki concentration after 24 hrs by dilution-offset filter binding assay | ChEMBL. | 21870878 |
Time (functional) | > 16 hr | Antagonist activity at M3 receptor in Dunkin-Hartley guinea pig tracheal strips assessed as time taken for electrically field-stimulated contractile response to recover by 25 percent of inhibition at Emax after 2 hrs | ChEMBL. | 21870878 |
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.