Assay Detail
Binding
CHEMBL856950
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Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.60 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41275 | — | — | 1 | 7.90 |
| CHEMBL432713 | — | — | 1 | 6.64 |
| CHEMBL131243 | — | — | 1 | 6.23 |
| CHEMBL337246 | — | — | 1 | 6.14 |
| CHEMBL134074 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41275 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL432713 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL131243 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL337246 | — | Ki | = | 724.44 | nM | 6.14 |
| CHEMBL134074 | — | Ki | = | 851.14 | nM | 6.07 |