Assay Detail
Functional
CHEMBL1108765
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Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.00 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092238 | — | — | 1 | 8.77 |
| CHEMBL1093802 | — | — | 1 | 8.59 |
| CHEMBL1089793 | — | — | 1 | 8.43 |
| CHEMBL1092921 | — | — | 1 | 7.96 |
| CHEMBL1088874 | — | — | 1 | 7.92 |
| CHEMBL1093469 | — | — | 1 | 7.75 |
| CHEMBL1089881 | — | — | 1 | 7.54 |
| CHEMBL1092929 | — | — | 1 | 7.52 |
| CHEMBL1093153 | — | — | 1 | 6.96 |
| CHEMBL1093470 | — | — | 1 | 6.92 |
| CHEMBL1092656 | — | — | 1 | 6.80 |
| CHEMBL1092343 | — | — | 1 | 6.77 |
| CHEMBL337246 | — | — | 1 | 6.52 |
| CHEMBL1090206 | — | — | 1 | 6.28 |
| CHEMBL1089965 | — | — | 1 | 6.21 |
| CHEMBL1089629 | — | — | 1 | 6.18 |
| CHEMBL1088810 | — | — | 1 | 6.15 |
| CHEMBL1090548 | — | — | 1 | 6.12 |
| CHEMBL255408 | — | — | 1 | 6.01 |
| CHEMBL1093154 | — | — | 1 | 5.96 |
| CHEMBL1090148 | — | — | 1 | 5.73 |
| CHEMBL1091171 | — | — | 1 | - |
| CHEMBL1091172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092238 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1093802 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1089793 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1092921 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1088874 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1093469 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1089881 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1092929 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1093153 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1093470 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1092656 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1092343 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL337246 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1090206 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1089965 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1089629 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1088810 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL1090548 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL255408 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL1093154 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1090148 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL1091171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1091172 | — | IC50 | > | 10000.0 | nM | - |