Assay Detail
Binding
CHEMBL1055929
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Displacement of human [125I]IL-8 from human CXCR2
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.79 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL560089 | — | — | 1 | 8.52 |
| CHEMBL557466 | — | — | 1 | 8.40 |
| CHEMBL254370 | — | — | 1 | 8.36 |
| CHEMBL562781 | — | — | 1 | 8.35 |
| CHEMBL563875 | — | — | 1 | 8.30 |
| CHEMBL385715 | — | — | 1 | 8.30 |
| CHEMBL556862 | — | — | 1 | 8.30 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 8.30 |
| CHEMBL564029 | — | — | 1 | 8.05 |
| CHEMBL563855 | — | — | 1 | 8.00 |
| CHEMBL561812 | — | — | 1 | 7.96 |
| CHEMBL562542 | — | — | 1 | 7.92 |
| CHEMBL562286 | — | — | 1 | 7.92 |
| CHEMBL550130 | — | — | 1 | 7.82 |
| CHEMBL557877 | — | — | 1 | 7.77 |
| CHEMBL556656 | — | — | 1 | 7.75 |
| CHEMBL556861 | — | — | 1 | 7.70 |
| CHEMBL562207 | — | — | 1 | 7.70 |
| CHEMBL550006 | — | — | 1 | 7.70 |
| CHEMBL551747 | — | — | 1 | 7.66 |
| CHEMBL559031 | — | — | 1 | 7.60 |
| CHEMBL562670 | — | — | 1 | 7.57 |
| CHEMBL563467 | — | — | 1 | 7.55 |
| CHEMBL564068 | — | — | 1 | 7.47 |
| CHEMBL550880 | — | — | 1 | 7.30 |
| CHEMBL562950 | — | — | 1 | 7.21 |
| CHEMBL550945 | — | — | 1 | 7.12 |
| CHEMBL563612 | — | — | 1 | 6.69 |
| CHEMBL563129 | — | — | 1 | 6.66 |
| CHEMBL550414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL560089 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL557466 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL254370 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL562781 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL563875 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL385715 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL556862 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL564029 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL563855 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL561812 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL562542 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL562286 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL550130 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL557877 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL556656 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL550006 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL562207 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL556861 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL551747 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL559031 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL562670 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL563467 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL564068 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL550880 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL562950 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL550945 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL563612 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL563129 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL550414 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL564862 | — | Ki | > | 270.0 | nM | - |
| CHEMBL561205 | — | Ki | > | 270.0 | nM | - |
| CHEMBL551748 | — | Ki | > | 270.0 | nM | - |
| CHEMBL564730 | — | Ki | > | 270.0 | nM | - |