Assay Detail
Binding
CHEMBL892289
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Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
31
Total Activities
31
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 | Expert |
Publication
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.05 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389293 | — | — | 1 | 8.15 |
| CHEMBL232441 | — | — | 1 | 8.00 |
| CHEMBL234295 | — | — | 1 | 7.92 |
| CHEMBL428193 | — | — | 1 | 7.82 |
| CHEMBL232837 | — | — | 1 | 7.75 |
| CHEMBL232638 | — | — | 1 | 7.70 |
| CHEMBL232253 | — | — | 1 | 7.60 |
| CHEMBL232654 | — | — | 1 | 7.58 |
| CHEMBL231829 | — | — | 1 | 7.58 |
| CHEMBL397910 | — | — | 1 | 7.38 |
| CHEMBL387608 | — | — | 1 | 7.30 |
| CHEMBL387822 | — | — | 1 | 7.20 |
| CHEMBL233042 | — | — | 1 | 7.19 |
| CHEMBL234073 | — | — | 1 | 7.14 |
| CHEMBL232655 | — | — | 1 | 7.12 |
| CHEMBL390706 | — | — | 1 | 7.11 |
| CHEMBL430356 | — | — | 1 | 7.05 |
| CHEMBL232043 | — | — | 1 | 7.01 |
| CHEMBL232455 | — | — | 1 | 6.85 |
| CHEMBL387821 | — | — | 1 | 6.80 |
| CHEMBL396700 | — | — | 1 | 6.80 |
| CHEMBL234081 | — | — | 1 | 6.77 |
| CHEMBL390707 | — | — | 1 | 6.70 |
| CHEMBL234276 | — | — | 1 | 6.66 |
| CHEMBL232042 | — | — | 1 | 6.57 |
| CHEMBL231830 | — | — | 1 | 6.46 |
| CHEMBL397956 | — | — | 1 | 6.10 |
| CHEMBL232252 | — | — | 1 | 6.04 |
| CHEMBL232044 | — | — | 1 | 5.63 |
| CHEMBL232251 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389293 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL232441 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL234295 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL428193 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL232837 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL232638 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL232253 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL232654 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL231829 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL397910 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL387608 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL387822 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL233042 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL234073 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL232655 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL390706 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL430356 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL232043 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL232455 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL387821 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL396700 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL234081 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL390707 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL234276 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL232042 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL231830 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL397956 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL232252 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL232044 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL232251 | — | IC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL233861 | — | IC50 | > | 10000.0 | nM | - |