Assay Detail
Functional
CHEMBL950882
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Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
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 | Autocuration |
Publication
Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.71 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232656 | BX 471 FREE BASE | 2.0 | 1 | 8.82 |
| CHEMBL475748 | — | — | 1 | 8.22 |
| CHEMBL473734 | — | — | 1 | 7.80 |
| CHEMBL514611 | — | — | 1 | 7.66 |
| CHEMBL473532 | — | — | 1 | 7.66 |
| CHEMBL473531 | — | — | 1 | 7.46 |
| CHEMBL517290 | — | — | 1 | 6.36 |
| CHEMBL461590 | — | — | 1 | - |
| CHEMBL516495 | — | — | 1 | - |
| CHEMBL462441 | — | — | 1 | - |
| CHEMBL462442 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232656 | BX 471 FREE BASE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL475748 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL473734 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL514611 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL473532 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL473531 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL517290 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL461590 | — | IC50 | - | — | - | |
| CHEMBL516495 | — | IC50 | - | — | - | |
| CHEMBL462441 | — | IC50 | - | — | - | |
| CHEMBL462442 | — | IC50 | - | — | - |