Assay Detail
Binding
CHEMBL904898
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Displacement of [125I]MCP1 from human CCR2 expressed in monocytes
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 8.08 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230281 | — | — | 1 | 9.37 |
| CHEMBL389771 | — | — | 1 | 9.10 |
| CHEMBL229316 | — | — | 1 | 8.89 |
| CHEMBL397749 | — | — | 1 | 8.89 |
| CHEMBL397948 | — | — | 1 | 8.85 |
| CHEMBL388487 | — | — | 1 | 8.77 |
| CHEMBL397996 | — | — | 1 | 8.74 |
| CHEMBL230790 | — | — | 1 | 8.74 |
| CHEMBL437552 | — | — | 1 | 8.64 |
| CHEMBL387583 | — | — | 1 | 8.59 |
| CHEMBL438304 | — | — | 1 | 8.52 |
| CHEMBL230166 | — | — | 1 | 8.52 |
| CHEMBL388486 | — | — | 1 | 8.52 |
| CHEMBL230684 | — | — | 1 | 8.46 |
| CHEMBL397997 | — | — | 1 | 8.46 |
| CHEMBL230794 | — | — | 1 | 8.41 |
| CHEMBL397747 | — | — | 1 | 8.40 |
| CHEMBL389888 | — | — | 1 | 8.28 |
| CHEMBL388868 | — | — | 1 | 8.24 |
| CHEMBL388867 | — | — | 1 | 8.19 |
| CHEMBL396517 | — | — | 1 | 8.14 |
| CHEMBL395721 | — | — | 1 | 8.13 |
| CHEMBL230727 | — | — | 1 | 8.04 |
| CHEMBL231340 | — | — | 1 | 7.89 |
| CHEMBL231252 | — | — | 1 | 7.89 |
| CHEMBL389773 | — | — | 1 | 7.88 |
| CHEMBL230507 | — | — | 1 | 7.88 |
| CHEMBL231149 | — | — | 1 | 7.85 |
| CHEMBL438514 | — | — | 1 | 7.84 |
| CHEMBL397750 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230281 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL389771 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL397749 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL229316 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL397948 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL388487 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL397996 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL230790 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL437552 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL387583 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL388486 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL230166 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL438304 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL230684 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL397997 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL230794 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL397747 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL389888 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL388868 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL388867 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL396517 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL395721 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL230727 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL231252 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL231340 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL389773 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL230507 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL231149 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL438514 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL397750 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL230165 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL388869 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL396101 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL438128 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL230624 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL395289 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL229536 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL398150 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL230791 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL230824 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL397717 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL388949 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL231150 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL427110 | — | IC50 | = | 182.7 | nM | 6.74 |
| CHEMBL230828 | — | IC50 | = | 229.0 | nM | 6.64 |