Assay Detail
Functional
CHEMBL1693607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
14
Total Activities
14
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
Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.02 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1688889 | — | — | 1 | 7.10 |
| CHEMBL1688888 | — | — | 1 | 6.16 |
| CHEMBL1687955 | — | — | 1 | 6.00 |
| CHEMBL1688879 | — | — | 1 | 5.82 |
| CHEMBL1688880 | — | — | 1 | 5.82 |
| CHEMBL1688878 | — | — | 1 | 5.80 |
| CHEMBL1688877 | — | — | 1 | 5.41 |
| CHEMBL1688881 | — | — | 1 | - |
| CHEMBL1688882 | — | — | 1 | - |
| CHEMBL1688883 | — | — | 1 | - |
| CHEMBL1688884 | — | — | 1 | - |
| CHEMBL1688885 | — | — | 1 | - |
| CHEMBL1688886 | — | — | 1 | - |
| CHEMBL1688887 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1688889 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1688888 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1687955 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1688879 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1688880 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1688878 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1688877 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1688881 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688882 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688883 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688884 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688885 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688886 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688887 | — | IC50 | > | 10000.0 | nM | - |