Assay Detail
Binding
CHEMBL2396023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
27
Total Activities
27
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
Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.23 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2332935 | — | — | 1 | 9.44 |
| CHEMBL2332936 | — | — | 1 | 9.28 |
| CHEMBL2391803 | — | — | 1 | 9.04 |
| CHEMBL2391810 | — | — | 1 | 8.96 |
| CHEMBL2391797 | — | — | 1 | 8.89 |
| CHEMBL2391939 | — | — | 1 | 8.85 |
| CHEMBL2391795 | — | — | 1 | 8.85 |
| CHEMBL2391808 | — | — | 1 | 8.74 |
| CHEMBL2391793 | — | — | 1 | 8.74 |
| CHEMBL2391804 | — | — | 1 | 8.72 |
| CHEMBL2391800 | — | — | 1 | 8.60 |
| CHEMBL2391938 | — | — | 1 | 8.60 |
| CHEMBL2391937 | — | — | 1 | 8.55 |
| CHEMBL2391794 | — | — | 1 | 8.49 |
| CHEMBL2391799 | — | — | 1 | 8.30 |
| CHEMBL2391809 | — | — | 1 | 8.15 |
| CHEMBL2391806 | — | — | 1 | 8.10 |
| CHEMBL2391796 | — | — | 1 | 8.10 |
| CHEMBL2391798 | — | — | 1 | 8.05 |
| CHEMBL2391802 | — | — | 1 | 7.92 |
| CHEMBL2391812 | — | — | 1 | 7.92 |
| CHEMBL2391811 | — | — | 1 | 7.50 |
| CHEMBL2391935 | — | — | 1 | 7.15 |
| CHEMBL2391807 | — | — | 1 | 7.05 |
| CHEMBL2391805 | — | — | 1 | 6.96 |
| CHEMBL2391801 | — | — | 1 | 6.89 |
| CHEMBL2391936 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2332935 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL2332936 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2391803 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL2391810 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2391797 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2391939 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2391795 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2391808 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2391793 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2391804 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2391800 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2391938 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2391937 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2391794 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2391799 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2391809 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2391806 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2391796 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2391798 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2391802 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2391812 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2391811 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2391935 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2391807 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2391805 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2391801 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2391936 | — | IC50 | = | 400.0 | nM | 6.40 |