Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | acetylcholinesterase (Yt blood group) | References | |
Homo sapiens | butyrylcholinesterase | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Carboxylesterase family protein | acetylcholinesterase (Yt blood group) | 614 aa | 510 aa | 26.5 % |
Brugia malayi | Carboxylesterase family protein | butyrylcholinesterase | 602 aa | 546 aa | 30.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.0164 | 0.5 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | carboxylesterase | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Brugia malayi | Carboxylesterase family protein | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | carboxylesterase 5A | 0.0164 | 0.5 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0164 | 0.5 | 0.5 |
Echinococcus multilocularis | carboxylesterase 5A | 0.0164 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 32.1 nM | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | ChEMBL. | 27309570 |
IC50 (binding) | = 3800 nM | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition by Ellman's method | ChEMBL. | 27309570 |
IC50 (binding) | > 50000 nM | Inhibition of FAAH in rat brain membrane using N-arachidonoyl-[14C]-ethanolamine as substrate incubated for 30 mins by scintillation counting method | ChEMBL. | 27309570 |
IC50 (binding) | > 50000 nM | Inhibition of FAAH in rat brain membrane using N-arachidonoyl-[14C]-ethanolamine as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by scintillation counting method | ChEMBL. | 27309570 |
Inhibition (binding) | Inhibition of human serum BuChE assessed as enzyme carbamoylation using butyrylthiocholine iodide as substrate preincubated with enzyme followed by substrate addition by Ellman's method | ChEMBL. | 27309570 | |
Inhibition (binding) | Inhibition of recombinant human AChE expressed in HEK293 cells assessed as enzyme carbamoylation using acetylthiocholine iodide as substrate preincubated with enzyme followed by substrate addition by Ellman's method | ChEMBL. | 27309570 | |
K (binding) | = 0.203 /min | Inhibition of recombinant human AChE expressed in HEK293 cells assessed as pseudo-first order rate constant for enzyme carbamoylation using acetylthiocholine iodide as substrate preincubated for 15 to 120 mins followed by substrate addition by Ellman's method | ChEMBL. | 27309570 |
K (binding) | = 0.461 /min | Inhibition of human serum BuChE assessed as pseudo-first order rate constant for enzyme carbamoylation using butyrylthiocholine iodide as substrate preincubated for 2 to 30 mins followed by substrate addition by Ellman's method | ChEMBL. | 27309570 |
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.