Assay Detail
Functional
CHEMBL1670538
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-1alpha-induced calcium mobilization Ca assay
9
Total Activities
9
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 | Autocuration |
Publication
Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.23 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1170878 | — | — | 1 | 7.89 |
| CHEMBL536743 | — | — | 1 | 7.55 |
| CHEMBL1668020 | — | — | 1 | 7.36 |
| CHEMBL1668022 | — | — | 1 | 7.29 |
| CHEMBL536754 | — | — | 1 | 7.28 |
| CHEMBL559168 | — | — | 1 | 7.08 |
| CHEMBL537424 | — | — | 1 | 7.03 |
| CHEMBL1668021 | — | — | 1 | 6.33 |
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1170878 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL536743 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1668020 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1668022 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL536754 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL559168 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL537424 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1668021 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | IC50 | = | 34.0 | nM | - |