Assay Detail
Binding
CHEMBL3579779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.24 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577945 | — | — | 1 | 9.62 |
| CHEMBL3577946 | — | — | 1 | 9.30 |
| CHEMBL3577942 | — | — | 1 | 9.22 |
| CHEMBL1091604 | — | — | 1 | 8.89 |
| CHEMBL3577940 | — | — | 1 | 8.74 |
| CHEMBL3577944 | — | — | 1 | 8.57 |
| CHEMBL3577937 | — | — | 1 | 8.57 |
| CHEMBL3577934 | — | — | 1 | 8.48 |
| CHEMBL3577943 | — | — | 1 | 8.48 |
| CHEMBL2018387 | — | — | 1 | 8.00 |
| CHEMBL3577939 | — | — | 1 | 7.80 |
| CHEMBL3577938 | — | — | 1 | 7.64 |
| CHEMBL3577935 | — | — | 1 | 7.60 |
| CHEMBL3577936 | — | — | 1 | 7.22 |
| CHEMBL3577941 | — | — | 1 | 7.12 |
| CHEMBL2018370 | — | — | 1 | 6.62 |
| CHEMBL3577933 | — | — | 1 | - |
| CHEMBL3577932 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577945 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3577946 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3577942 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1091604 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3577940 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3577944 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3577937 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3577934 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3577943 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2018387 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3577939 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3577938 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3577935 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3577936 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3577941 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2018370 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3577933 | — | IC50 | < | 0.45 | nM | - |
| CHEMBL3577932 | — | IC50 | < | 0.45 | nM | - |