Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | histamine receptor H3 | Starlite/ChEMBL | References |
Rattus norvegicus | Acetylcholinesterase | Starlite/ChEMBL | References |
Homo sapiens | histamine receptor H4 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus multilocularis | neuroligin | Acetylcholinesterase | 614 aa | 496 aa | 24.0 % |
Echinococcus multilocularis | BC026374 protein (S09 family) | Acetylcholinesterase | 614 aa | 642 aa | 34.0 % |
Onchocerca volvulus | Acetylcholinesterase | 614 aa | 581 aa | 27.0 % | |
Onchocerca volvulus | Acetylcholinesterase | 614 aa | 583 aa | 30.7 % | |
Onchocerca volvulus | Acetylcholinesterase | 614 aa | 632 aa | 25.6 % | |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | Acetylcholinesterase | 614 aa | 602 aa | 24.3 % |
Drosophila melanogaster | CG10175 gene product from transcript CG10175-RE | Acetylcholinesterase | 614 aa | 547 aa | 32.5 % |
Onchocerca volvulus | Molybdopterin synthase catalytic subunit homolog | Acetylcholinesterase | 614 aa | 564 aa | 29.8 % |
Loa Loa (eye worm) | hypothetical protein | Acetylcholinesterase | 614 aa | 574 aa | 24.0 % |
Onchocerca volvulus | Putative nuclear protein | Acetylcholinesterase | 614 aa | 577 aa | 40.7 % |
Echinococcus granulosus | BC026374 protein S09 family | Acetylcholinesterase | 614 aa | 642 aa | 34.1 % |
Brugia malayi | Carboxylesterase family protein | Acetylcholinesterase | 614 aa | 507 aa | 26.4 % |
Onchocerca volvulus | Carnitine O-palmitoyltransferase 2, mitochondrial homolog | Acetylcholinesterase | 614 aa | 531 aa | 39.7 % |
Brugia malayi | Carboxylesterase family protein | Acetylcholinesterase | 614 aa | 573 aa | 30.5 % |
Loa Loa (eye worm) | hypothetical protein | Acetylcholinesterase | 614 aa | 570 aa | 25.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.0014 | 0 | 0.5 | |
Loa Loa (eye worm) | hypothetical protein | 0.0082 | 0.6586 | 0.6586 |
Echinococcus multilocularis | acetylcholinesterase | 0.0082 | 0.6586 | 1 |
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.0082 | 0.6586 | 0.6586 |
Entamoeba histolytica | hypothetical protein | 0.0035 | 0.2078 | 0.5 |
Schistosoma mansoni | transcription factor LCR-F1 | 0.0035 | 0.2078 | 0.3155 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription | 0.0035 | 0.2078 | 0.3155 |
Trichomonas vaginalis | carboxylesterase domain containing protein, putative | 0.0014 | 0 | 0.5 |
Entamoeba histolytica | hypothetical protein | 0.0035 | 0.2078 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0082 | 0.6586 | 0.6586 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription | 0.0035 | 0.2078 | 0.3155 |
Onchocerca volvulus | 0.0014 | 0 | 0.5 | |
Loa Loa (eye worm) | MH2 domain-containing protein | 0.0117 | 1 | 1 |
Brugia malayi | Carboxylesterase family protein | 0.0082 | 0.6586 | 0.6586 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0082 | 0.6586 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0035 | 0.2078 | 0.5 |
Onchocerca volvulus | 0.0014 | 0 | 0.5 | |
Onchocerca volvulus | 0.0014 | 0 | 0.5 | |
Loa Loa (eye worm) | carboxylesterase | 0.0082 | 0.6586 | 0.6586 |
Schistosoma mansoni | hypothetical protein | 0.0035 | 0.2078 | 0.3155 |
Trichomonas vaginalis | spcc417.12 protein, putative | 0.0014 | 0 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0082 | 0.6586 | 1 |
Mycobacterium tuberculosis | POSSIBLE PARA-NITROBENZYL ESTERASE (FRAGMENT) | 0.0014 | 0 | 0.5 |
Brugia malayi | Carboxylesterase family protein | 0.0082 | 0.6586 | 0.6586 |
Mycobacterium tuberculosis | POSSIBLE PARA-NITROBENZYL ESTERASE (FRAGMENT) | 0.0014 | 0 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.0082 | 0.6586 | 1 |
Onchocerca volvulus | 0.0014 | 0 | 0.5 | |
Entamoeba histolytica | hypothetical protein | 0.0035 | 0.2078 | 0.5 |
Echinococcus multilocularis | carboxylesterase 5A | 0.0082 | 0.6586 | 1 |
Echinococcus multilocularis | acetylcholinesterase | 0.0082 | 0.6586 | 1 |
Mycobacterium ulcerans | carboxylesterase, LipT | 0.0014 | 0 | 0.5 |
Echinococcus granulosus | carboxylesterase 5A | 0.0082 | 0.6586 | 1 |
Loa Loa (eye worm) | transcription factor SMAD2 | 0.0117 | 1 | 1 |
Brugia malayi | hypothetical protein | 0.0035 | 0.2078 | 0.2078 |
Mycobacterium tuberculosis | Carboxylesterase LipT | 0.0014 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 170.6 nM | Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 |
IC50 (functional) | = 511 nM | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 |
IC50 (binding) | = 0.313 uM | Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | ChEMBL. | 22019465 |
IC50 (functional) | > 10 uM | Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 |
Inhibition (functional) | Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 | |
Inhibition (functional) | Antagonist activity at histamine H2 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 | |
Inhibition (functional) | Antagonist activity at histamine H1 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 | |
Inhibition (binding) | = 44.79 % | Inhibition of BACE1 at 20 ug/mL by FRET assay | ChEMBL. | 22019465 |
Inhibition (functional) | = 65.3 % | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | ChEMBL. | 22019465 |
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.