Assay Detail
Binding
CHEMBL890113
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Displacement of [125I]MIP1-alpha from human CCR5 expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.88 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL536754 | — | — | 1 | 8.96 |
| CHEMBL559168 | — | — | 1 | 8.46 |
| CHEMBL536743 | — | — | 1 | 8.21 |
| CHEMBL537424 | — | — | 1 | 8.08 |
| CHEMBL556995 | — | — | 1 | 7.96 |
| CHEMBL557789 | — | — | 1 | 7.62 |
| CHEMBL535172 | — | — | 1 | 7.55 |
| CHEMBL536298 | — | — | 1 | 7.54 |
| CHEMBL558043 | — | — | 1 | 7.28 |
| CHEMBL536751 | — | — | 1 | 7.17 |
| CHEMBL538336 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL536754 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL559168 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL536743 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL537424 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL556995 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL557789 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL535172 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL536298 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL558043 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL536751 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL538336 | — | IC50 | - | — | - |