Assay Detail
Binding
CHEMBL2038472
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
38
Total Activities
38
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
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.98 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2036782 | — | — | 1 | 8.46 |
| CHEMBL2036755 | — | — | 1 | 8.30 |
| CHEMBL2036757 | — | — | 1 | 8.00 |
| CHEMBL2036758 | — | — | 1 | 7.80 |
| CHEMBL2036760 | — | — | 1 | 7.77 |
| CHEMBL2036775 | — | — | 1 | 7.77 |
| CHEMBL2036780 | — | — | 1 | 7.68 |
| CHEMBL2036777 | — | — | 1 | 7.58 |
| CHEMBL2036762 | — | — | 1 | 7.57 |
| CHEMBL2036781 | — | — | 1 | 7.50 |
| CHEMBL2036761 | — | — | 1 | 7.46 |
| CHEMBL2036751 | — | — | 1 | 7.43 |
| CHEMBL2036759 | — | — | 1 | 7.30 |
| CHEMBL2036754 | — | — | 1 | 7.28 |
| CHEMBL2036764 | — | — | 1 | 7.24 |
| CHEMBL2036773 | — | — | 1 | 7.19 |
| CHEMBL2036756 | — | — | 1 | 7.19 |
| CHEMBL2036767 | — | — | 1 | 7.17 |
| CHEMBL2036783 | — | — | 1 | 7.16 |
| CHEMBL2036766 | — | — | 1 | 7.01 |
| CHEMBL2036753 | — | — | 1 | 7.00 |
| CHEMBL2036750 | — | — | 1 | 6.91 |
| CHEMBL2035000 | — | — | 1 | 6.90 |
| CHEMBL2036748 | — | — | 1 | 6.77 |
| CHEMBL2036763 | — | — | 1 | 6.77 |
| CHEMBL2036774 | — | — | 1 | 6.57 |
| CHEMBL2036769 | — | — | 1 | 6.35 |
| CHEMBL2036772 | — | — | 1 | 6.15 |
| CHEMBL2036749 | — | — | 1 | 6.11 |
| CHEMBL2036776 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2036782 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2036755 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2036757 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2036758 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2036760 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2036775 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2036780 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2036777 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2036762 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2036781 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2036761 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2036751 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2036759 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2036754 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2036764 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2036773 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2036756 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2036767 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2036783 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2036766 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2036753 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2036750 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL2035000 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL2036748 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2036763 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL2036774 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL2036769 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL2036772 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2036749 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2036776 | — | IC50 | = | 797.0 | nM | 6.10 |
| CHEMBL2036778 | — | IC50 | = | 856.0 | nM | 6.07 |
| CHEMBL2036768 | — | IC50 | = | 1055.0 | nM | 5.98 |
| CHEMBL2036752 | — | IC50 | = | 1184.0 | nM | 5.93 |
| CHEMBL2036765 | — | IC50 | = | 1458.0 | nM | 5.84 |
| CHEMBL2036779 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL2036784 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2036770 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2036771 | — | IC50 | > | 10000.0 | nM | - |