Assay Detail
Functional
CHEMBL892290
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Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 11 | 8.01 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232441 | — | — | 1 | 8.40 |
| CHEMBL387608 | — | — | 1 | 8.30 |
| CHEMBL389293 | — | — | 1 | 8.22 |
| CHEMBL232837 | — | — | 1 | 8.22 |
| CHEMBL397910 | — | — | 1 | 8.10 |
| CHEMBL234295 | — | — | 1 | 7.92 |
| CHEMBL232638 | — | — | 1 | 7.89 |
| CHEMBL232253 | — | — | 1 | 7.85 |
| CHEMBL231829 | — | — | 1 | 7.75 |
| CHEMBL232656 | BX 471 FREE BASE | 2.0 | 1 | 7.75 |
| CHEMBL387822 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232441 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL387608 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL389293 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL232837 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL397910 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL234295 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL232638 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL232253 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL231829 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL232656 | BX 471 FREE BASE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL387822 | — | IC50 | = | 19.0 | nM | 7.72 |