Species | Target name | Source | Bibliographic reference |
---|---|---|---|
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 |
---|---|---|---|---|
Toxoplasma gondii | hypothetical protein | 0.0093 | 0 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.0093 | 0 | 0.5 |
Trypanosoma brucei | glutaminyl cyclase, putative | 0.0093 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0093 | 0 | 0.5 |
Mycobacterium ulcerans | hypothetical protein | 0.0093 | 0 | 0.5 |
Leishmania major | glutaminyl cyclase, putative | 0.0093 | 0 | 0.5 |
Mycobacterium ulcerans | lipoprotein aminopeptidase LpqL | 0.0093 | 0 | 0.5 |
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | 0.0586 | 1 | 1 |
Mycobacterium tuberculosis | Probable lipoprotein aminopeptidase LpqL | 0.0093 | 0 | 0.5 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0093 | 0 | 0.5 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | 0.0586 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0586 | 1 | 1 |
Onchocerca volvulus | Glutaminyl cyclase homolog | 0.0586 | 1 | 1 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0093 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0093 | 0 | 0.5 |
Trichomonas vaginalis | Clan MH, family M28, aminopeptidase S-like metallopeptidase | 0.0093 | 0 | 0.5 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0093 | 0 | 0.5 |
Toxoplasma gondii | peptidase, M28 family protein | 0.0093 | 0 | 0.5 |
Schistosoma mansoni | glutaminyl cyclase (M28 family) | 0.0586 | 1 | 1 |
Mycobacterium tuberculosis | Conserved protein | 0.0093 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
-Log Ki (binding) | = 4 | Binding affinity of the compound against H2 receptor of Guinea pig atrium | ChEMBL. | 8676353 |
-Log Ki (binding) | < 4 | Binding affinity of the compound against H1 receptor of Guinea pig ileum | ChEMBL. | 8676353 |
-Log Ki (binding) | = 7.9 | Binding affinity of the compound against Histamine H3 receptor on Synaptosomes from rat cerebral cortex was evaluated | ChEMBL. | 8676353 |
ED50 (functional) | = 10 mg kg-1 | In vivo antagonistic activity against Histamine H3 receptor in mouse after peroral administration was assessed from the brain histamine turnover | ChEMBL. | 8676353 |
ED50 (functional) | = 10 mg kg-1 | In vivo antagonistic activity against Histamine H3 receptor in mouse after peroral administration was assessed from the brain histamine turnover | ChEMBL. | 8676353 |
Ki (binding) | = 4 | Binding affinity of the compound against H2 receptor of Guinea pig atrium | ChEMBL. | 8676353 |
Ki (binding) | > 4 | Binding affinity of the compound against H1 receptor of Guinea pig ileum | ChEMBL. | 8676353 |
Ki (binding) | = 7.9 | Binding affinity of the compound against Histamine H3 receptor on Synaptosomes from rat cerebral cortex was evaluated | ChEMBL. | 8676353 |
Ki (functional) | = 14 nM | In vitro antagonistic activity of the compound against Histamine H3 receptor on Synaptosomes of rat cerebral cortex. | ChEMBL. | 8676353 |
Ki (functional) | = 14 nM | In vitro antagonistic activity of the compound against Histamine H3 receptor on Synaptosomes of rat cerebral cortex. | ChEMBL. | 8676353 |
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.