Assay Detail
Functional
CHEMBL1930241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.27 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1926899 | — | — | 1 | 10.05 |
| CHEMBL1926893 | — | — | 1 | 9.70 |
| CHEMBL1927008 | — | — | 1 | 9.52 |
| CHEMBL1927009 | — | — | 1 | 9.52 |
| CHEMBL1926896 | — | — | 1 | 9.52 |
| CHEMBL1926898 | — | — | 1 | 9.52 |
| CHEMBL1926900 | — | — | 1 | 9.22 |
| CHEMBL1927010 | — | — | 1 | 9.15 |
| CHEMBL1926891 | — | — | 1 | 9.15 |
| CHEMBL1926901 | — | — | 1 | 9.10 |
| CHEMBL1926904 | — | — | 1 | 9.01 |
| CHEMBL1926902 | — | — | 1 | 8.89 |
| CHEMBL1926894 | — | — | 1 | 8.82 |
| CHEMBL1926897 | — | — | 1 | 8.80 |
| CHEMBL1926885 | — | — | 1 | 8.70 |
| CHEMBL1926890 | — | — | 1 | 8.62 |
| CHEMBL1926884 | — | — | 1 | 8.52 |
| CHEMBL1926886 | — | — | 1 | 8.52 |
| CHEMBL1926889 | — | — | 1 | 8.15 |
| CHEMBL1926905 | — | — | 1 | 8.15 |
| CHEMBL1926883 | — | — | 1 | 8.10 |
| CHEMBL1926888 | — | — | 1 | 7.96 |
| CHEMBL1926878 | — | — | 1 | 7.96 |
| CHEMBL1926887 | — | — | 1 | 7.92 |
| CHEMBL1926892 | — | — | 1 | 7.91 |
| CHEMBL1926875 | — | — | 1 | 7.72 |
| CHEMBL1926874 | — | — | 1 | 7.58 |
| CHEMBL1926880 | — | — | 1 | 7.52 |
| CHEMBL1926872 | — | — | 1 | 7.47 |
| CHEMBL1926895 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1926899 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL1926893 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1927009 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1926896 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1926898 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1927008 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1926900 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1927010 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1926891 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1926901 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1926904 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL1926902 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1926894 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1926897 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1926885 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1926890 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1926884 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1926886 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1926889 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1926905 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1926883 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1926888 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL1926878 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1926887 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1926892 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL1926875 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1926874 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1926880 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1926872 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1926895 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1762313 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1926873 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1926876 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1926877 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1926903 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1926882 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL1927007 | — | IC50 | = | 1586.0 | nM | 5.80 |