Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium voltage-gated channel, subfamily H (eag-related), member 2 | Starlite/ChEMBL | References |
Homo sapiens | histamine receptor H3 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 0.96 nM | Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding | ChEMBL. | 18598020 |
IC50 (binding) | = 2600 nM | Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay | ChEMBL. | 21802950 |
IC50 (binding) | = 2.6 uM | Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthalenyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-6-yl]methanesulfonamide from human ERG in HEK293 cells | ChEMBL. | 18598020 |
Ki (binding) | = 0.3125 nM | Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assay | ChEMBL. | 21802950 |
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.