Assay Detail
Binding
CHEMBL864277
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Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.31 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441856 | — | — | 1 | 8.40 |
| CHEMBL215020 | — | — | 1 | 8.05 |
| CHEMBL378195 | — | — | 1 | 7.92 |
| CHEMBL213058 | — | — | 1 | 7.89 |
| CHEMBL385540 | — | — | 1 | 7.82 |
| CHEMBL380190 | — | — | 1 | 7.43 |
| CHEMBL215394 | — | — | 1 | 7.43 |
| CHEMBL215654 | — | — | 1 | 7.42 |
| CHEMBL214641 | — | — | 1 | 7.38 |
| CHEMBL215093 | — | — | 1 | 7.33 |
| CHEMBL214825 | — | — | 1 | 7.32 |
| CHEMBL215689 | — | — | 1 | 7.14 |
| CHEMBL214647 | — | — | 1 | 7.14 |
| CHEMBL214747 | — | — | 1 | 7.14 |
| CHEMBL212972 | — | — | 1 | 7.10 |
| CHEMBL215391 | — | — | 1 | 7.07 |
| CHEMBL409162 | — | — | 1 | 7.03 |
| CHEMBL215759 | — | — | 1 | 6.89 |
| CHEMBL215271 | — | — | 1 | 6.67 |
| CHEMBL212939 | — | — | 1 | 6.63 |
| CHEMBL377819 | — | — | 1 | 6.33 |
| CHEMBL386711 | — | — | 1 | - |
| CHEMBL215976 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441856 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL215020 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL378195 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL213058 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL385540 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL380190 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL215394 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL215654 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL214641 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL215093 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL214825 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL215689 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL214647 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL214747 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL212972 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL215391 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL409162 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL215759 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL215271 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL212939 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL377819 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL386711 | — | IC50 | - | — | - | |
| CHEMBL215976 | — | IC50 | - | — | - |