Assay Detail
Binding
CHEMBL929862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]IL8 from human CXCR2 by SPA assay
24
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.23 | 9.00 |
| IC50 | 2 | 8.24 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254175 | — | — | 1 | 9.00 |
| CHEMBL402965 | — | — | 1 | 8.82 |
| CHEMBL404074 | — | — | 1 | 8.77 |
| CHEMBL254775 | — | — | 1 | 8.77 |
| CHEMBL254176 | — | — | 1 | 8.72 |
| CHEMBL404918 | — | — | 1 | 8.72 |
| CHEMBL254174 | — | — | 1 | 8.55 |
| CHEMBL254982 | — | — | 1 | 8.36 |
| CHEMBL254776 | — | — | 1 | 8.35 |
| CHEMBL254370 | — | — | 2 | 8.33 |
| CHEMBL401512 | — | — | 2 | 8.31 |
| CHEMBL254173 | — | — | 1 | 8.28 |
| CHEMBL254570 | — | — | 1 | 8.21 |
| CHEMBL254980 | — | — | 1 | 8.10 |
| CHEMBL404073 | — | — | 1 | 7.93 |
| CHEMBL404917 | — | — | 1 | 7.92 |
| CHEMBL254981 | — | — | 1 | 7.88 |
| CHEMBL254369 | — | — | 1 | 7.86 |
| CHEMBL254571 | — | — | 1 | 7.80 |
| CHEMBL254368 | — | — | 1 | 7.71 |
| CHEMBL254172 | — | — | 1 | 7.55 |
| CHEMBL254572 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254175 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL402965 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL404074 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL254775 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL254176 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL404918 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL254174 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL254982 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL254776 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL254370 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL401512 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL254173 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL254570 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL254370 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL254980 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL401512 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL404073 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL404917 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL254981 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL254369 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL254571 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL254368 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL254172 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL254572 | — | Ki | = | 38.5 | nM | 7.42 |