Assay Detail
Binding
CHEMBL3366539
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Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
17
Total Activities
17
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
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.18 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3334817 | — | — | 1 | 8.70 |
| CHEMBL3334725 | — | — | 1 | 8.52 |
| CHEMBL3334728 | — | — | 1 | 8.40 |
| CHEMBL3334815 | — | — | 1 | 8.22 |
| CHEMBL3334816 | — | — | 1 | 8.22 |
| CHEMBL3334824 | BMS-817399 | 2.0 | 1 | 8.22 |
| CHEMBL3334823 | — | — | 1 | 8.22 |
| CHEMBL3334821 | — | — | 1 | 8.15 |
| CHEMBL3334727 | — | — | 1 | 8.00 |
| CHEMBL3334726 | — | — | 1 | 7.72 |
| CHEMBL3334825 | — | — | 1 | 7.66 |
| CHEMBL3334820 | — | — | 1 | - |
| CHEMBL3334822 | — | — | 1 | - |
| CHEMBL3334819 | — | — | 1 | - |
| CHEMBL2398716 | — | — | 1 | - |
| CHEMBL3334818 | — | — | 1 | - |
| CHEMBL3334724 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3334817 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3334725 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3334728 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3334815 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334816 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334824 | BMS-817399 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334823 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334821 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334727 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3334726 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3334825 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3334820 | — | IC50 | - | — | - | |
| CHEMBL3334822 | — | IC50 | - | — | - | |
| CHEMBL3334819 | — | IC50 | - | — | - | |
| CHEMBL2398716 | — | IC50 | - | — | - | |
| CHEMBL3334818 | — | IC50 | - | — | - | |
| CHEMBL3334724 | — | IC50 | - | — | - |