Assay Detail
Functional
CHEMBL1687494
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CXCR3
59
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 6.96 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1681882 | — | — | 1 | 9.70 |
| CHEMBL472288 | — | — | 1 | 9.52 |
| CHEMBL1681868 | — | — | 1 | 8.64 |
| CHEMBL1681870 | — | — | 1 | 8.62 |
| CHEMBL1681874 | — | — | 1 | 8.52 |
| CHEMBL1681869 | — | — | 1 | 8.30 |
| CHEMBL1681832 | — | — | 2 | 8.30 |
| CHEMBL1681849 | — | — | 1 | 8.22 |
| CHEMBL1681865 | — | — | 1 | 8.10 |
| CHEMBL1681850 | — | — | 1 | 7.80 |
| CHEMBL1681833 | — | — | 1 | 7.77 |
| CHEMBL1681835 | — | — | 1 | 7.75 |
| CHEMBL1681866 | — | — | 1 | 7.70 |
| CHEMBL1681871 | — | — | 1 | 7.66 |
| CHEMBL1681883 | — | — | 1 | 7.64 |
| CHEMBL1681856 | — | — | 1 | 7.57 |
| CHEMBL1681844 | — | — | 2 | 7.54 |
| CHEMBL1681855 | — | — | 1 | 7.51 |
| CHEMBL1681841 | — | — | 1 | 7.50 |
| CHEMBL1681884 | — | — | 1 | 7.50 |
| CHEMBL578779 | — | — | 1 | 7.46 |
| CHEMBL1681851 | — | — | 1 | 7.41 |
| CHEMBL1681867 | — | — | 1 | 7.41 |
| CHEMBL1681848 | — | — | 1 | 7.40 |
| CHEMBL1681843 | — | — | 1 | 7.24 |
| CHEMBL1681834 | — | — | 1 | 7.20 |
| CHEMBL1681854 | — | — | 1 | 7.19 |
| CHEMBL1681863 | — | — | 1 | 7.10 |
| CHEMBL1681864 | — | — | 1 | 7.08 |
| CHEMBL1681836 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1681882 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL472288 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1681868 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1681870 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1681874 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1681869 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1681832 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1681849 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1681865 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1681850 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1681833 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1681835 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1681866 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1681871 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1681883 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1681856 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1681844 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1681855 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1681884 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1681841 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL578779 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1681844 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1681851 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1681867 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1681848 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1681843 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1681834 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1681854 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1681863 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1681864 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1681836 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1681832 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1681877 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1681845 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1681852 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1681875 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1681861 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1681862 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL565761 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1681873 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1681876 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1681872 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1681878 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1681857 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1681840 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL1681853 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1681879 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL570509 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1681858 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1681860 | — | IC50 | = | 7350.0 | nM | 5.13 |