Assay Detail
Binding
CHEMBL886375
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Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA
21
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.48 | 9.22 |
| IC50 | 1 | 8.89 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL396573 | — | — | 1 | 9.22 |
| CHEMBL246318 | — | — | 1 | 9.10 |
| CHEMBL246108 | — | — | 2 | 9.00 |
| CHEMBL245699 | — | — | 1 | 9.00 |
| CHEMBL246941 | — | — | 1 | 8.70 |
| CHEMBL246106 | — | — | 1 | 8.70 |
| CHEMBL247150 | — | — | 1 | 8.52 |
| CHEMBL246731 | — | — | 1 | 8.52 |
| CHEMBL246733 | — | — | 1 | 8.40 |
| CHEMBL245501 | — | — | 1 | 8.40 |
| CHEMBL394899 | — | — | 1 | 8.40 |
| CHEMBL247149 | — | — | 1 | 8.40 |
| CHEMBL247356 | — | — | 1 | 8.40 |
| CHEMBL393900 | — | — | 1 | 8.30 |
| CHEMBL415446 | — | — | 1 | 8.30 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 8.30 |
| CHEMBL442799 | — | — | 1 | 8.22 |
| CHEMBL246107 | — | — | 1 | 8.05 |
| CHEMBL245500 | — | — | 1 | 8.00 |
| CHEMBL245697 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL396573 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL246318 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL245699 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL246108 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL246108 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL246941 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL246106 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL246731 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL247150 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL394899 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL245501 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL247356 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL247149 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL246733 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL393900 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL415446 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL442799 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL246107 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL245500 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL245697 | — | Ki | = | 25.0 | nM | 7.60 |