Assay Detail
Functional
CHEMBL940862
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Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.31 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247245 | — | — | 1 | 8.10 |
| CHEMBL246804 | — | — | 1 | 7.43 |
| CHEMBL247621 | — | — | 1 | 7.28 |
| CHEMBL400196 | — | — | 1 | 7.28 |
| CHEMBL392814 | — | — | 1 | 7.24 |
| CHEMBL247455 | — | — | 1 | 7.24 |
| CHEMBL247608 | — | — | 1 | 7.24 |
| CHEMBL248418 | — | — | 1 | 7.16 |
| CHEMBL398747 | — | — | 1 | 7.09 |
| CHEMBL393267 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247245 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL246804 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL247621 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL400196 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL392814 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL247455 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL247608 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL248418 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL398747 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL393267 | — | IC50 | = | 84.0 | nM | 7.08 |