Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Equus caballus | Cholinesterase | References | |
Homo sapiens | butyrylcholinesterase | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Carboxylesterase family protein | Cholinesterase | 574 aa | 549 aa | 29.5 % |
Onchocerca volvulus | Cholinesterase | 574 aa | 551 aa | 29.9 % | |
Loa Loa (eye worm) | hypothetical protein | Cholinesterase | 574 aa | 520 aa | 27.1 % |
Loa Loa (eye worm) | hypothetical protein | Cholinesterase | 574 aa | 573 aa | 26.4 % |
Onchocerca volvulus | Cholinesterase | 574 aa | 578 aa | 25.3 % | |
Echinococcus multilocularis | BC026374 protein (S09 family) | Cholinesterase | 574 aa | 636 aa | 34.9 % |
Onchocerca volvulus | Molybdopterin synthase catalytic subunit homolog | Cholinesterase | 574 aa | 560 aa | 29.3 % |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | Cholinesterase | 574 aa | 590 aa | 25.1 % |
Echinococcus granulosus | BC026374 protein S09 family | Cholinesterase | 574 aa | 642 aa | 34.4 % |
Onchocerca volvulus | Putative nuclear protein | Cholinesterase | 574 aa | 572 aa | 40.9 % |
Drosophila melanogaster | CG10175 gene product from transcript CG10175-RE | Cholinesterase | 574 aa | 547 aa | 29.4 % |
Onchocerca volvulus | Galectin homolog | Cholinesterase | 574 aa | 531 aa | 39.7 % |
Brugia malayi | Carboxylesterase family protein | butyrylcholinesterase | 602 aa | 546 aa | 30.2 % |
Schistosoma mansoni | gliotactin | Cholinesterase | 574 aa | 587 aa | 27.9 % |
Onchocerca volvulus | Carnitine O-palmitoyltransferase 2, mitochondrial homolog | Cholinesterase | 574 aa | 554 aa | 36.1 % |
Brugia malayi | Carboxylesterase family protein | Cholinesterase | 574 aa | 538 aa | 31.4 % |
Schistosoma japonicum | ko:K01050 cholinesterase [EC3.1.1.8], putative | Cholinesterase | 574 aa | 577 aa | 36.9 % |
Echinococcus granulosus | neuroligin | Cholinesterase | 574 aa | 492 aa | 24.4 % |
Echinococcus multilocularis | neuroligin | Cholinesterase | 574 aa | 493 aa | 26.2 % |
Brugia malayi | Carboxylesterase family protein | Cholinesterase | 574 aa | 472 aa | 27.5 % |
Onchocerca volvulus | Cholinesterase | 574 aa | 586 aa | 27.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
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 |
Loa Loa (eye worm) | carboxylesterase | 0.0164 | 0.5 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Brugia malayi | Carboxylesterase family protein | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | carboxylesterase 5A | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0164 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0164 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.013 uM | Inhibition of human butyrylcholinesterase using butyrylcholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 2.5 mins by Ellman's spectrophotometric method | ChEMBL. | 26886849 |
IC50 (binding) | = 0.014 uM | Inhibition of equine serum butyrylcholinesterase using butyrylcholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 2.5 mins by Ellman's spectrophotometric method | ChEMBL. | 26886849 |
Inhibition (binding) | = 0 % | Inhibition of human acetylcholinesterase using acetylcholine iodide as substrate at 100 uM preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's spectrophotometric method | ChEMBL. | 26886849 |
K (binding) | = 0.14 /hr | Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as decarbamoylation rate using butyrylcholine iodide as substrate preincubated for 1 hr followed by 1000 fold dilution | ChEMBL. | 26886849 |
K (binding) | = 0.14 /min | Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as carbamoylation rate of inhibitor from reversible enzyme inhibitor complex to carbamoylated enzyme using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
K (binding) | = 0.32 /min | Pseudo-irreversible inhibition of human butyrylcholinesterase assessed as carbamoylation rate of inhibitor from reversible enzyme inhibitor complex to carbamoylated enzyme using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
K (binding) | = 14.3 nM | Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
K (binding) | = 19.7 nM | Pseudo-irreversible inhibition of human butyrylcholinesterase assessed as apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
Ratio (binding) | = 9.79 /uM/min | Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as ratio of carbamoylation rate of inhibitor to apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
Ratio (binding) | = 16.24 /uM/min | Pseudo-irreversible inhibition of human butyrylcholinesterase assessed as ratio of carbamoylation rate of inhibitor to apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by double reciprocal plot analysis | ChEMBL. | 26886849 |
T1/2 (binding) | = 5 hr | Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as half life for carbamoylated enzyme using butyrylcholine iodide as substrate preincubated for 1 hr followed by 1000 fold dilution | ChEMBL. | 26886849 |
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.