Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | histamine receptor H3 | Starlite/ChEMBL | References |
Rattus norvegicus | Histamine H3 receptor | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | biogenic amine 5HT receptor | Histamine H3 receptor | 445 aa | 405 aa | 25.2 % |
Loa Loa (eye worm) | hypothetical protein | Histamine H3 receptor | 445 aa | 384 aa | 22.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | carboxylesterase 5A | 0.0398 | 1 | 1 |
Trypanosoma cruzi | polo-like protein kinase, putative | 0.0092 | 0.1543 | 0.5 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0067 | 0.0845 | 0.0577 |
Giardia lamblia | Kinase, PLK | 0.0092 | 0.1543 | 0.5 |
Trypanosoma cruzi | polo-like protein kinase, putative | 0.0092 | 0.1543 | 0.5 |
Loa Loa (eye worm) | carboxylesterase | 0.0067 | 0.0845 | 0.0495 |
Brugia malayi | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Echinococcus granulosus | acetylcholinesterase | 0.0398 | 1 | 1 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Echinococcus multilocularis | neuroligin | 0.0067 | 0.0845 | 0.0845 |
Schistosoma mansoni | neuroligin 3 (S09 family) | 0.0067 | 0.0845 | 0.0577 |
Mycobacterium tuberculosis | POSSIBLE PARA-NITROBENZYL ESTERASE (FRAGMENT) | 0.0067 | 0.0845 | 0.5 |
Echinococcus multilocularis | serine:threonine protein kinase PLK1 | 0.0092 | 0.1543 | 0.1543 |
Leishmania major | protein kinase, putative,polo-like protein kinase, putative | 0.0092 | 0.1543 | 1 |
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.0398 | 1 | 1 |
Brugia malayi | Carboxylesterase family protein | 0.0067 | 0.0845 | 0.0495 |
Schistosoma mansoni | gliotactin | 0.0067 | 0.0845 | 0.0577 |
Brugia malayi | Carboxylesterase family protein | 0.0398 | 1 | 1 |
Echinococcus granulosus | acetylcholinesterase | 0.0398 | 1 | 1 |
Echinococcus granulosus | serine:threonine protein kinase PLK1 | 0.0092 | 0.1543 | 0.1543 |
Loa Loa (eye worm) | carboxylesterase | 0.0398 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0067 | 0.0845 | 0.0577 |
Loa Loa (eye worm) | PLK/PLK1 protein kinase | 0.0092 | 0.1543 | 0.122 |
Trichomonas vaginalis | carboxylesterase domain containing protein, putative | 0.0067 | 0.0845 | 0.4597 |
Echinococcus multilocularis | family S9 non peptidase ue (S09 family) | 0.0067 | 0.0845 | 0.0845 |
Mycobacterium ulcerans | carboxylesterase, LipT | 0.0067 | 0.0845 | 0.5 |
Entamoeba histolytica | serine/threonine protein kinase, putative | 0.0092 | 0.1543 | 0.5 |
Echinococcus granulosus | para nitrobenzyl esterase | 0.0067 | 0.0845 | 0.0845 |
Echinococcus granulosus | neuroligin | 0.0067 | 0.0845 | 0.0845 |
Echinococcus granulosus | family S9 non peptidase ue S09 family | 0.0067 | 0.0845 | 0.0845 |
Echinococcus granulosus | geminin | 0.0168 | 0.3638 | 0.3638 |
Brugia malayi | Carboxylesterase family protein | 0.0067 | 0.0845 | 0.0495 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Schistosoma mansoni | acetylcholinesterase | 0.0067 | 0.0845 | 0.0577 |
Loa Loa (eye worm) | carboxylesterase | 0.0067 | 0.0845 | 0.0495 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Schistosoma mansoni | BC026374 protein (S09 family) | 0.0067 | 0.0845 | 0.0577 |
Echinococcus granulosus | carboxylesterase 5A | 0.0398 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0398 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0092 | 0.1543 | 0.1296 |
Trichomonas vaginalis | spcc417.12 protein, putative | 0.0067 | 0.0845 | 0.4597 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Brugia malayi | serine/threonine-protein kinase plk-2 | 0.0092 | 0.1543 | 0.122 |
Schistosoma mansoni | hypothetical protein | 0.0168 | 0.3638 | 0.3452 |
Echinococcus multilocularis | para nitrobenzyl esterase | 0.0067 | 0.0845 | 0.0845 |
Mycobacterium tuberculosis | POSSIBLE PARA-NITROBENZYL ESTERASE (FRAGMENT) | 0.0067 | 0.0845 | 0.5 |
Mycobacterium tuberculosis | Carboxylesterase LipT | 0.0067 | 0.0845 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.0398 | 1 | 1 |
Brugia malayi | Carboxylesterase family protein | 0.0067 | 0.0845 | 0.0495 |
Echinococcus multilocularis | geminin | 0.0168 | 0.3638 | 0.3638 |
Echinococcus multilocularis | BC026374 protein (S09 family) | 0.0067 | 0.0845 | 0.0845 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Echinococcus multilocularis | acetylcholinesterase | 0.0398 | 1 | 1 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0398 | 1 | 1 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Onchocerca volvulus | Serine\/threonine kinase homolog | 0.0092 | 0.1543 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0168 | 0.3638 | 0.3452 |
Echinococcus granulosus | BC026374 protein S09 family | 0.0067 | 0.0845 | 0.0845 |
Brugia malayi | Carboxylesterase family protein | 0.0067 | 0.0845 | 0.0495 |
Loa Loa (eye worm) | hypothetical protein | 0.0398 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0067 | 0.0845 | 0.0495 |
Trypanosoma brucei | polo-like protein kinase | 0.0092 | 0.1543 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0092 | 0.1543 | 1 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.0067 | 0.0845 | 0.0577 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 7.43 | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | ChEMBL. | 21928839 |
Ki (functional) | = 8.05 | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | ChEMBL. | 21928839 |
Ki (binding) | = 8.64 | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | ChEMBL. | 21928839 |
Ki (functional) | = 8.77 | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | ChEMBL. | 21928839 |
Ki (functional) | = 1.7 nM | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | ChEMBL. | 21928839 |
Ki (binding) | = 2.3 nM | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | ChEMBL. | 21928839 |
Ki (functional) | = 8.9 nM | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | ChEMBL. | 21928839 |
Ki (binding) | = 37 nM | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | ChEMBL. | 21928839 |
permeability (ADMET) | = 44.7 ucm/s | Permeability across apical to basolateral side in human Caco2 cells at 2 uM | ChEMBL. | 21928839 |
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.