Assay Detail
Functional
CHEMBL1670539
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Antagonist activity at human CCR5 expressed in HOS cells assessed as inhibition of cell fusion with HIV gp120 expressing HEK293 cells by LTR luciferase assay
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HOS |
| 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 | 8 | 6.96 | 8.25 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | 3.0 | 1 | 8.25 |
| CHEMBL536754 | — | — | 1 | 8.11 |
| CHEMBL1170878 | — | — | 1 | 7.06 |
| CHEMBL1668020 | — | — | 1 | 6.74 |
| CHEMBL559168 | — | — | 1 | 6.64 |
| CHEMBL1668021 | — | — | 1 | 6.42 |
| CHEMBL1668022 | — | — | 1 | 6.35 |
| CHEMBL537424 | — | — | 1 | 6.07 |
| CHEMBL536743 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | IC50 | = | 5.623 | nM | 8.25 |
| CHEMBL536754 | — | IC50 | = | 7.762 | nM | 8.11 |
| CHEMBL1170878 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL1668020 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL559168 | — | IC50 | = | 229.09 | nM | 6.64 |
| CHEMBL1668021 | — | IC50 | = | 380.19 | nM | 6.42 |
| CHEMBL1668022 | — | IC50 | = | 446.68 | nM | 6.35 |
| CHEMBL537424 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL536743 | — | pIC50 | - | — | - |