Assay Detail
Binding
CHEMBL863683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cells
29
Total Activities
29
Compounds Tested
3
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
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.58 | 8.10 |
| Ki | 2 | 7.42 | 7.54 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380258 | — | — | 1 | 8.10 |
| CHEMBL209411 | — | — | 1 | 8.00 |
| CHEMBL209063 | — | — | 1 | 7.89 |
| CHEMBL208685 | — | — | 1 | 7.60 |
| CHEMBL376981 | — | — | 1 | 7.54 |
| CHEMBL209263 | — | — | 1 | 7.50 |
| CHEMBL211775 | — | — | 1 | 7.41 |
| CHEMBL432713 | — | — | 1 | 7.30 |
| CHEMBL210606 | — | — | 1 | 6.76 |
| CHEMBL427396 | — | — | 1 | 6.70 |
| CHEMBL209267 | — | — | 1 | 6.66 |
| CHEMBL378995 | — | — | 1 | 6.47 |
| CHEMBL212306 | — | — | 1 | 6.40 |
| CHEMBL379818 | — | — | 1 | 6.37 |
| CHEMBL209171 | — | — | 1 | 6.28 |
| CHEMBL379278 | — | — | 1 | 6.24 |
| CHEMBL212674 | — | — | 1 | 6.23 |
| CHEMBL378517 | — | — | 1 | 6.17 |
| CHEMBL209002 | — | — | 1 | 6.12 |
| CHEMBL378784 | — | — | 1 | 6.11 |
| CHEMBL211404 | — | — | 1 | 6.08 |
| CHEMBL212423 | — | — | 1 | 6.08 |
| CHEMBL211292 | — | — | 1 | 6.06 |
| CHEMBL211560 | — | — | 1 | 6.00 |
| CHEMBL378658 | — | — | 1 | 5.83 |
| CHEMBL377432 | — | — | 1 | 4.87 |
| CHEMBL376958 | — | — | 1 | - |
| CHEMBL209412 | — | — | 1 | - |
| CHEMBL211668 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380258 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL209411 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL209063 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL208685 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL376981 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL209263 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL211775 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL432713 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL210606 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL427396 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL209267 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL378995 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL212306 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL379818 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL209171 | — | IC50 | = | 521.0 | nM | 6.28 |
| CHEMBL379278 | — | IC50 | = | 575.0 | nM | 6.24 |
| CHEMBL212674 | — | IC50 | = | 592.0 | nM | 6.23 |
| CHEMBL378517 | — | IC50 | = | 678.0 | nM | 6.17 |
| CHEMBL209002 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL378784 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL211404 | — | IC50 | = | 838.0 | nM | 6.08 |
| CHEMBL212423 | — | IC50 | = | 822.0 | nM | 6.08 |
| CHEMBL211292 | — | IC50 | = | 865.0 | nM | 6.06 |
| CHEMBL211560 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL378658 | — | IC50 | = | 1477.0 | nM | 5.83 |
| CHEMBL377432 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL376958 | — | IC50 | = | - | % | - |
| CHEMBL209412 | — | IC50 | = | - | % | - |
| CHEMBL211668 | — | Inhibition | = | 1100.0 | nM | - |