Assay Detail
Functional
CHEMBL1001497
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Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.13 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497202 | — | — | 1 | 9.52 |
| CHEMBL502247 | — | — | 1 | 9.30 |
| CHEMBL502793 | — | — | 1 | 9.15 |
| CHEMBL496630 | — | — | 1 | 8.82 |
| CHEMBL502516 | — | — | 1 | 8.29 |
| CHEMBL499467 | — | — | 1 | 8.19 |
| CHEMBL496432 | — | — | 1 | 8.12 |
| CHEMBL450231 | — | — | 1 | 7.80 |
| CHEMBL273083 | — | — | 1 | 7.75 |
| CHEMBL502515 | — | — | 1 | 7.68 |
| CHEMBL502795 | — | — | 1 | 7.68 |
| CHEMBL447937 | — | — | 1 | 7.62 |
| CHEMBL452509 | — | — | 1 | 7.47 |
| CHEMBL442929 | — | — | 1 | 7.42 |
| CHEMBL451597 | — | — | 1 | 7.19 |
| CHEMBL451340 | — | — | 1 | - |
| CHEMBL496632 | — | — | 1 | - |
| CHEMBL448989 | — | — | 1 | - |
| CHEMBL500786 | — | — | 1 | - |
| CHEMBL502248 | — | — | 1 | - |
| CHEMBL526180 | — | — | 1 | - |
| CHEMBL500175 | — | — | 1 | - |
| CHEMBL526752 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497202 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL502247 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL502793 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL496630 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL502516 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL499467 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL496432 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL450231 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL273083 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL502515 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL502795 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL447937 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL452509 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL442929 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL451597 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL451340 | — | IC50 | - | — | - | |
| CHEMBL496632 | — | IC50 | - | — | - | |
| CHEMBL448989 | — | IC50 | - | — | - | |
| CHEMBL500786 | — | IC50 | - | — | - | |
| CHEMBL502248 | — | IC50 | - | — | - | |
| CHEMBL526180 | — | IC50 | - | — | - | |
| CHEMBL500175 | — | IC50 | - | — | - | |
| CHEMBL526752 | — | IC50 | - | — | - |