Assay Detail
Functional
CHEMBL1108767
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Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
11
Total Activities
11
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 | Autocuration |
Publication
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.65 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088874 | — | — | 1 | 8.05 |
| CHEMBL1093469 | — | — | 1 | 8.05 |
| CHEMBL1089793 | — | — | 1 | 8.00 |
| CHEMBL1092929 | — | — | 1 | 7.64 |
| CHEMBL1092238 | — | — | 1 | 7.64 |
| CHEMBL337246 | — | — | 1 | 7.16 |
| CHEMBL495202 | — | — | 1 | 7.00 |
| CHEMBL255408 | — | — | 1 | - |
| CHEMBL1089881 | — | — | 1 | - |
| CHEMBL1092921 | — | — | 1 | - |
| CHEMBL1093802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088874 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1093469 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1089793 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1092929 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1092238 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL337246 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL495202 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL255408 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL1089881 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL1092921 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL1093802 | — | IC50 | > | 100.0 | nM | - |