Assay Detail
Functional
CHEMBL1104171
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Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.24 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1077828 | — | — | 1 | 8.30 |
| CHEMBL1077824 | — | — | 1 | 8.00 |
| CHEMBL1077831 | — | — | 1 | 7.82 |
| CHEMBL1077817 | — | — | 1 | 7.77 |
| CHEMBL1077827 | — | — | 1 | 7.70 |
| CHEMBL1077826 | — | — | 1 | 7.70 |
| CHEMBL1077819 | — | — | 1 | 7.70 |
| CHEMBL404201 | — | — | 1 | 7.70 |
| CHEMBL1077830 | — | — | 1 | 7.66 |
| CHEMBL1077820 | — | — | 1 | 7.64 |
| CHEMBL1077832 | — | — | 1 | 7.24 |
| CHEMBL1077823 | — | — | 1 | 7.23 |
| CHEMBL1075640 | — | — | 1 | 7.12 |
| CHEMBL1077825 | — | — | 1 | 7.10 |
| CHEMBL253431 | — | — | 1 | 6.94 |
| CHEMBL1081164 | — | — | 1 | 6.88 |
| CHEMBL230664 | — | — | 1 | 6.85 |
| CHEMBL1077829 | — | — | 1 | 6.79 |
| CHEMBL1077818 | — | — | 1 | 6.66 |
| CHEMBL397983 | — | — | 1 | 6.62 |
| CHEMBL436826 | — | — | 1 | 6.46 |
| CHEMBL1077809 | — | — | 1 | 6.35 |
| CHEMBL1077810 | — | — | 1 | 6.30 |
| CHEMBL1077812 | — | — | 1 | - |
| CHEMBL1077822 | — | — | 1 | - |
| CHEMBL1077811 | — | — | 1 | - |
| CHEMBL1077821 | — | — | 1 | - |
| CHEMBL1077813 | — | — | 1 | - |
| CHEMBL1077808 | — | — | 1 | - |
| CHEMBL1077807 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1077828 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1077824 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1077831 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1077817 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1077827 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1077826 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1077819 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL404201 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1077830 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1077820 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1077832 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1077823 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1075640 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1077825 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL253431 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL1081164 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL230664 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1077829 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1077818 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL397983 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL436826 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1077809 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1077810 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1077812 | — | IC50 | - | — | - | |
| CHEMBL1077822 | — | IC50 | - | — | - | |
| CHEMBL1077811 | — | IC50 | - | — | - | |
| CHEMBL1077821 | — | IC50 | - | — | - | |
| CHEMBL1077813 | — | IC50 | - | — | - | |
| CHEMBL1077808 | — | IC50 | - | — | - | |
| CHEMBL1077807 | — | IC50 | - | — | - | |
| CHEMBL1077814 | — | IC50 | - | — | - | |
| CHEMBL1077815 | — | IC50 | - | — | - | |
| CHEMBL1077816 | — | IC50 | - | — | - |