Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Histamine H3 receptor | Starlite/ChEMBL | References |
Homo sapiens | histamine receptor H3 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | Histamine H3 receptor | 445 aa | 384 aa | 22.4 % |
Echinococcus granulosus | biogenic amine 5HT receptor | Histamine H3 receptor | 445 aa | 405 aa | 25.2 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells at upto 10 uM | ChEMBL. | 18976927 | |
Activity (functional) | Antagonist activity at histamine H1 receptor in guinea pig terminal ileum at upto 10 uM | ChEMBL. | 18976927 | |
Activity (functional) | Antagonist activity at histamine H2 receptor in guinea pig atrium assessed as changes in rate of spontaneous beat at upto 10 uM | ChEMBL. | 18976927 | |
Activity (functional) | Activity at histamine H2 receptor in isolated guinea pig atrium up to 10 uM | ChEMBL. | 16713264 | |
Activity (functional) | Activity at histamine H1 receptor in isolated guinea pig ileum up to 10 uM | ChEMBL. | 16713264 | |
Activity (binding) | Inhibition of acetylcholinesterase in Wistar rat brain homogenate at upto 10 uM by Ellman's method | ChEMBL. | 18976927 | |
Activity (functional) | Activity at histamine H3 receptor assessed as RAMHA-induced inhibition of electrically-stimulated guinea pig isolated ileum | ChEMBL. | 16713264 | |
Activity (functional) | 0 | Activity at histamine H3 receptor assessed as RAMHA-induced inhibition of electrically-stimulated guinea pig isolated ileum | ChEMBL. | 16713264 |
Activity (functional) | 0 | Activity at histamine H2 receptor in isolated guinea pig atrium up to 10 uM | ChEMBL. | 16713264 |
Activity (functional) | 0 | Activity at histamine H1 receptor in isolated guinea pig ileum up to 10 uM | ChEMBL. | 16713264 |
Ki (binding) | = -7.91 | Displacement of [3H]RAMHA from human histamine H3 receptor transfected in SK-N-MC cells | ChEMBL. | 16713264 |
Ki (binding) | = -7.09 | Displacement of [3H]RAMHA from histamine H3 receptor in rat brain membranes | ChEMBL. | 16713264 |
Ki (binding) | = 7.09 | Displacement of [3H]RAMHA from histamine H3 receptor in Wistar rat brain membrane | ChEMBL. | 18976927 |
Ki (binding) | = 7.91 | Displacement of [3H]RAMHA from human histamine H3 receptor expressed in SK-N-MC cells | ChEMBL. | 18976927 |
Log Ki (binding) | = 7.09 | Displacement of [3H]RAMHA from histamine H3 receptor in rat brain membranes | ChEMBL. | 16713264 |
Log Ki (binding) | = 7.91 | Displacement of [3H]RAMHA from human histamine H3 receptor transfected in SK-N-MC cells | ChEMBL. | 16713264 |
pKb (functional) | Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced twitch contraction in presence of 1 uM mepyramine | ChEMBL. | 18976927 | |
pKb (functional) | = 7.67 | Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells by CRE-mediated beta-galactosidase reporter gene assay administered 10 mins before (R)-alpha-methylhistamine challenge after 6 hrs | ChEMBL. | 18976927 |
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.
2 literature references were collected for this gene.