Assay Detail
Binding
CHEMBL4715396
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Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.79 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764460 | — | — | 1 | 9.52 |
| CHEMBL4790208 | — | — | 1 | 9.22 |
| CHEMBL4442783 | — | — | 1 | 9.15 |
| CHEMBL4781426 | — | — | 1 | 9.10 |
| CHEMBL4757857 | — | — | 1 | 8.80 |
| CHEMBL4760098 | — | — | 1 | 8.77 |
| CHEMBL4757452 | — | — | 1 | 8.52 |
| CHEMBL4741305 | — | — | 1 | 8.35 |
| CHEMBL4742683 | — | — | 1 | 7.70 |
| CHEMBL4746510 | — | — | 1 | - |
| CHEMBL4760566 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764460 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4790208 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4442783 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4781426 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4757857 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4760098 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4757452 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4741305 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4742683 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4746510 | — | IC50 | - | — | - | |
| CHEMBL4760566 | — | IC50 | - | — | - |