Assay Detail
Binding
CHEMBL949060
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Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Evaluation of a series of bicyclic CXCR2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.62 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403225 | — | — | 1 | 9.00 |
| CHEMBL256668 | — | — | 1 | 9.00 |
| CHEMBL446458 | — | — | 1 | 9.00 |
| CHEMBL272105 | — | — | 1 | 8.70 |
| CHEMBL271012 | — | — | 1 | 8.70 |
| CHEMBL429791 | — | — | 1 | 8.52 |
| CHEMBL397237 | — | — | 1 | 8.40 |
| CHEMBL272705 | — | — | 1 | 8.30 |
| CHEMBL429682 | — | — | 1 | 8.30 |
| CHEMBL402986 | — | — | 1 | 8.30 |
| CHEMBL271703 | — | — | 1 | 8.15 |
| CHEMBL257006 | — | — | 1 | 7.89 |
| CHEMBL271013 | — | — | 1 | 7.89 |
| CHEMBL232846 | — | — | 1 | 7.89 |
| CHEMBL403656 | — | — | 1 | 7.80 |
| CHEMBL233263 | — | — | 1 | 7.46 |
| CHEMBL403877 | — | — | 1 | 7.35 |
| CHEMBL402728 | — | — | 1 | 7.22 |
| CHEMBL390191 | — | — | 1 | 6.92 |
| CHEMBL403702 | — | — | 1 | 6.85 |
| CHEMBL257025 | — | — | 1 | 6.66 |
| CHEMBL257659 | — | — | 1 | 6.55 |
| CHEMBL404057 | — | — | 1 | 6.55 |
| CHEMBL257269 | — | — | 1 | 6.46 |
| CHEMBL270446 | — | — | 1 | 6.20 |
| CHEMBL258334 | — | — | 1 | 6.07 |
| CHEMBL257027 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403225 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL256668 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL446458 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL272105 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL271012 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL429791 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL397237 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL272705 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL429682 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL402986 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL271703 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL257006 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL271013 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL232846 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL403656 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL233263 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL403877 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL402728 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL390191 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL403702 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL257025 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL257659 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL404057 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL257269 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL270446 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL258334 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL257027 | — | IC50 | = | 2500.0 | nM | 5.60 |