Assay Detail
Functional
CHEMBL929487
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Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.68 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL271828 | — | — | 1 | 8.43 |
| CHEMBL270959 | — | — | 1 | 8.32 |
| CHEMBL273083 | — | — | 1 | 7.75 |
| CHEMBL411726 | — | — | 1 | 7.52 |
| CHEMBL270906 | — | — | 1 | 7.38 |
| CHEMBL272168 | — | — | 1 | 6.67 |
| CHEMBL272167 | — | — | 1 | - |
| CHEMBL429425 | — | — | 1 | - |
| CHEMBL411935 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL271828 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL270959 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL273083 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL411726 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL270906 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL272168 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL272167 | — | IC50 | - | — | - | |
| CHEMBL429425 | — | IC50 | - | — | - | |
| CHEMBL411935 | — | IC50 | - | — | - |