Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium voltage-gated channel, subfamily H (eag-related), member 2 | Starlite/ChEMBL | References |
Homo sapiens | chemokine (C-C motif) receptor 2 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 6.2 nM | Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting | ChEMBL. | 21295478 |
IC50 (functional) | = 6.2 nM | Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins | ChEMBL. | 21295478 |
IC50 (functional) | = 18.8 nM | Antagonist activity at human CCR2 by whole blood assay | ChEMBL. | 21315584 |
IC50 (binding) | = 26.5 nM | Displacement of labeled MIP-1beta from human CCR5 receptor | ChEMBL. | 21295478 |
IC50 (binding) | = 27.5 nM | Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay | ChEMBL. | 21315584 |
IC50 (binding) | = 79 nM | Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry | ChEMBL. | 21295478 |
IC50 (binding) | = 3.9 uM | Displacement of labeled dofetilide from human ERG | ChEMBL. | 21315584 |
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.