Assay Detail
Binding
CHEMBL863111
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Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 32 | 6.71 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441856 | — | — | 1 | 7.85 |
| CHEMBL215020 | — | — | 1 | 7.60 |
| CHEMBL378195 | — | — | 1 | 7.55 |
| CHEMBL213601 | — | — | 1 | 7.17 |
| CHEMBL215654 | — | — | 1 | 7.16 |
| CHEMBL277279 | — | — | 1 | 7.10 |
| CHEMBL213058 | — | — | 1 | 7.10 |
| CHEMBL385540 | — | — | 1 | 7.01 |
| CHEMBL214641 | — | — | 1 | 6.90 |
| CHEMBL211923 | — | — | 1 | 6.90 |
| CHEMBL214747 | — | — | 1 | 6.80 |
| CHEMBL409162 | — | — | 1 | 6.76 |
| CHEMBL210606 | — | — | 1 | 6.75 |
| CHEMBL215394 | — | — | 1 | 6.71 |
| CHEMBL215093 | — | — | 1 | 6.69 |
| CHEMBL380190 | — | — | 1 | 6.64 |
| CHEMBL212542 | — | — | 1 | 6.61 |
| CHEMBL214647 | — | — | 1 | 6.55 |
| CHEMBL215759 | — | — | 1 | 6.54 |
| CHEMBL212939 | — | — | 1 | 6.53 |
| CHEMBL215689 | — | — | 1 | 6.46 |
| CHEMBL379634 | — | — | 1 | 6.36 |
| CHEMBL378258 | — | — | 1 | 6.28 |
| CHEMBL378449 | — | — | 1 | 6.24 |
| CHEMBL215391 | — | — | 1 | 6.22 |
| CHEMBL215271 | — | — | 1 | 6.19 |
| CHEMBL212972 | — | — | 1 | 6.18 |
| CHEMBL378784 | — | — | 1 | 6.14 |
| CHEMBL215768 | — | — | 1 | 6.11 |
| CHEMBL215333 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441856 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL215020 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL378195 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL213601 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL215654 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL277279 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL213058 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL385540 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL214641 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL211923 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL214747 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL409162 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL210606 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL215394 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL215093 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL380190 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL212542 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL214647 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL215759 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL212939 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL215689 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL379634 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL378258 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL378449 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL215391 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL215271 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL212972 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL378784 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL215768 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL215333 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL377819 | — | IC50 | - | — | - | |
| CHEMBL214825 | — | IC50 | - | — | - |