Assay Detail
Binding
CHEMBL3579780
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Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-1080 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.59 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577945 | — | — | 1 | 8.62 |
| CHEMBL3577946 | — | — | 1 | 8.52 |
| CHEMBL3577942 | — | — | 1 | 8.47 |
| CHEMBL3577948 | — | — | 1 | 8.00 |
| CHEMBL3577949 | — | — | 1 | 7.75 |
| CHEMBL3577944 | — | — | 1 | 7.66 |
| CHEMBL3577932 | — | — | 1 | 6.86 |
| CHEMBL3577933 | — | — | 1 | 6.49 |
| CHEMBL3577934 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577945 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3577946 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3577942 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3577948 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3577949 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3577944 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3577932 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3577933 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL3577934 | — | IC50 | = | 1242.0 | nM | 5.91 |