Assay Detail
Functional
CHEMBL890112
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CCR5 expressed in CHO cells assessed as inhibition of MIP-1-alpha-stimulated calcium mobilization
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 10 | 7.03 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL536743 | — | — | 1 | 7.55 |
| CHEMBL559168 | — | — | 1 | 7.48 |
| CHEMBL536754 | — | — | 1 | 7.28 |
| CHEMBL535172 | — | — | 1 | 7.10 |
| CHEMBL556995 | — | — | 1 | 7.08 |
| CHEMBL537424 | — | — | 1 | 7.03 |
| CHEMBL536298 | — | — | 1 | 6.89 |
| CHEMBL558043 | — | — | 1 | 6.82 |
| CHEMBL557789 | — | — | 1 | 6.68 |
| CHEMBL536751 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL536743 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL559168 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL536754 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL535172 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL556995 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL537424 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL536298 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL558043 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL557789 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL536751 | — | IC50 | = | 400.0 | nM | 6.40 |