Assay Detail
Binding
CHEMBL869238
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Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
21
Total Activities
21
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
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.46 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385824 | — | — | 1 | 7.35 |
| CHEMBL213601 | — | — | 1 | 7.23 |
| CHEMBL277279 | — | — | 1 | 7.10 |
| CHEMBL373491 | — | — | 1 | 6.92 |
| CHEMBL211092 | — | — | 1 | 6.85 |
| CHEMBL209899 | — | — | 1 | 6.82 |
| CHEMBL215515 | — | — | 1 | 6.80 |
| CHEMBL210606 | — | — | 1 | 6.75 |
| CHEMBL209267 | — | — | 1 | 6.66 |
| CHEMBL212928 | — | — | 1 | 6.50 |
| CHEMBL213648 | — | — | 1 | 6.36 |
| CHEMBL379742 | — | — | 1 | 6.16 |
| CHEMBL378784 | — | — | 1 | 6.14 |
| CHEMBL209696 | — | — | 1 | 6.11 |
| CHEMBL212423 | — | — | 1 | 6.08 |
| CHEMBL386865 | — | — | 1 | 6.03 |
| CHEMBL209975 | — | — | 1 | 6.00 |
| CHEMBL211106 | — | — | 1 | 5.97 |
| CHEMBL384368 | — | — | 1 | 5.96 |
| CHEMBL379624 | — | — | 1 | 5.96 |
| CHEMBL209423 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385824 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL213601 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL277279 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL373491 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL211092 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL209899 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL215515 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL210606 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL209267 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL212928 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL213648 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL379742 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL378784 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL209696 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL212423 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL386865 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL209975 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL211106 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL384368 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL379624 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL209423 | — | IC50 | = | 1500.0 | nM | 5.82 |