Assay Detail
Binding
CHEMBL4371835
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 chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimization of pyrazole amides as antagonists of CCR1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.04 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232656 | BX 471 FREE BASE | 2.0 | 1 | 8.96 |
| CHEMBL3334824 | BMS-817399 | 2.0 | 1 | 8.82 |
| CHEMBL4571977 | — | — | 1 | 8.74 |
| CHEMBL4444976 | CCX354 | 2.0 | 1 | 8.40 |
| CHEMBL1628706 | — | — | 1 | 7.41 |
| CHEMBL4539264 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232656 | BX 471 FREE BASE | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3334824 | BMS-817399 | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4571977 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4444976 | CCX354 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1628706 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4539264 | — | IC50 | = | 1200.0 | nM | 5.92 |