Assay Detail
Functional
CHEMBL5033752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.32 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3819292 | — | — | 1 | 7.89 |
| CHEMBL5088269 | — | — | 1 | 7.47 |
| CHEMBL5081049 | — | — | 1 | 7.37 |
| CHEMBL5076154 | — | — | 1 | 7.31 |
| CHEMBL5078788 | — | — | 1 | 7.18 |
| CHEMBL5070965 | — | — | 1 | 7.11 |
| CHEMBL5093947 | — | — | 1 | 7.02 |
| CHEMBL5089441 | — | — | 1 | 6.89 |
| CHEMBL5088825 | — | — | 1 | 6.85 |
| CHEMBL5090244 | — | — | 1 | 6.82 |
| CHEMBL5090422 | — | — | 1 | 6.72 |
| CHEMBL5078730 | — | — | 1 | 6.70 |
| CHEMBL5087256 | — | — | 1 | 6.68 |
| CHEMBL5083131 | — | — | 1 | 6.68 |
| CHEMBL5071577 | — | — | 1 | 6.50 |
| CHEMBL5089049 | — | — | 1 | 6.43 |
| CHEMBL5079979 | — | — | 1 | 6.40 |
| CHEMBL5080880 | — | — | 1 | 6.38 |
| CHEMBL5081756 | — | — | 1 | 6.16 |
| CHEMBL5083610 | — | — | 1 | 5.99 |
| CHEMBL5076384 | — | — | 1 | 5.98 |
| CHEMBL5078087 | — | — | 1 | 5.88 |
| CHEMBL5083848 | — | — | 1 | 5.87 |
| CHEMBL5076418 | — | — | 1 | 5.83 |
| CHEMBL5081113 | — | — | 1 | 5.80 |
| CHEMBL5086977 | — | — | 1 | 5.79 |
| CHEMBL5075434 | — | — | 1 | 5.61 |
| CHEMBL5092474 | — | — | 1 | 5.60 |
| CHEMBL5087298 | — | — | 1 | 5.46 |
| CHEMBL5094410 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3819292 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5088269 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5081049 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5076154 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5078788 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5070965 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5093947 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5089441 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5088825 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5090244 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5090422 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5078730 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5087256 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5083131 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5071577 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5089049 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5079979 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5080880 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5081756 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5083610 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5076384 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5078087 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL5083848 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5076418 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5081113 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5086977 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL5075434 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL5092474 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5087298 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL5094410 | — | IC50 | = | 4510.0 | nM | 5.35 |
| CHEMBL5075579 | — | IC50 | = | 5920.0 | nM | 5.23 |
| CHEMBL5084752 | — | IC50 | = | 9990.0 | nM | 5.00 |
| CHEMBL5078246 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5079554 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5094132 | — | IC50 | > | 10000.0 | nM | - |