Assay Detail
Binding
CHEMBL893601
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Displacement of [125I]IL8 from human CXCR2 expressed in HEK 293 by SPA
25
Total Activities
25
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 | Expert |
Publication
SAR studies on thiazolo[4,5-d]pyrimidine based CXCR2 antagonists involving a novel tandem displacement reaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.39 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429791 | — | — | 1 | 8.40 |
| CHEMBL397237 | — | — | 1 | 8.40 |
| CHEMBL245180 | — | — | 1 | 8.10 |
| CHEMBL394799 | — | — | 1 | 7.90 |
| CHEMBL232846 | — | — | 1 | 7.90 |
| CHEMBL389791 | — | — | 1 | 7.80 |
| CHEMBL233260 | — | — | 1 | 7.80 |
| CHEMBL233059 | — | — | 1 | 7.80 |
| CHEMBL396043 | — | — | 1 | 7.70 |
| CHEMBL380947 | — | — | 1 | 7.60 |
| CHEMBL380732 | — | — | 1 | 7.60 |
| CHEMBL233259 | — | — | 1 | 7.50 |
| CHEMBL233263 | — | — | 1 | 7.50 |
| CHEMBL437013 | — | — | 1 | 7.50 |
| CHEMBL245190 | — | — | 1 | 7.50 |
| CHEMBL414894 | — | — | 1 | 7.20 |
| CHEMBL389792 | — | — | 1 | 7.10 |
| CHEMBL395340 | — | — | 1 | 7.00 |
| CHEMBL430381 | — | — | 1 | 7.00 |
| CHEMBL233262 | — | — | 1 | 7.00 |
| CHEMBL390191 | — | — | 1 | 6.90 |
| CHEMBL395342 | — | — | 1 | 6.40 |
| CHEMBL233264 | — | — | 1 | 6.00 |
| CHEMBL245182 | — | — | 1 | 5.80 |
| CHEMBL243862 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429791 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL397237 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL245180 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL394799 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL232846 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL389791 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL233260 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL233059 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL396043 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL380947 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL380732 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL233259 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL233263 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL437013 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL245190 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL414894 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL389792 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL395340 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL430381 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL233262 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL390191 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL395342 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL233264 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL245182 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL243862 | — | IC50 | < | 1000.0 | nM | - |