Assay Detail
Functional
CHEMBL3591343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Chem-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.44 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41275 | — | — | 1 | 9.02 |
| CHEMBL3589952 | — | — | 1 | 7.77 |
| CHEMBL3589845 | — | — | 1 | 7.05 |
| CHEMBL3588870 | — | — | 1 | 6.79 |
| CHEMBL3589847 | — | — | 1 | 6.76 |
| CHEMBL3589842 | — | — | 1 | 6.75 |
| CHEMBL3589844 | — | — | 1 | 6.50 |
| CHEMBL3589950 | — | — | 1 | 6.45 |
| CHEMBL3589846 | — | — | 1 | 6.33 |
| CHEMBL3589839 | — | — | 1 | 6.17 |
| CHEMBL3589841 | — | — | 1 | 5.91 |
| CHEMBL3589949 | — | — | 1 | 5.80 |
| CHEMBL3589951 | — | — | 1 | 5.21 |
| CHEMBL3589840 | — | — | 1 | 5.12 |
| CHEMBL3589843 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41275 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3589952 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3589845 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3588870 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL3589847 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3589842 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3589844 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL3589950 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL3589846 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL3589839 | — | IC50 | = | 684.0 | nM | 6.17 |
| CHEMBL3589841 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL3589949 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3589951 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3589840 | — | IC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL3589843 | — | IC50 | = | 12000.0 | nM | 4.92 |