Assay Detail
Binding
CHEMBL5162230
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human CXCR2 expressed in human U87 cells assessed as inhibition of CXCL8 AF647-binding incubated for 15 mins followed by addition of CXCL8 AF647 measured after 30 mins by flow cytometry analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U87 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.47 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397237 | — | — | 1 | 7.89 |
| CHEMBL5195797 | — | — | 1 | 7.89 |
| CHEMBL5173775 | — | — | 1 | 7.36 |
| CHEMBL5186932 | — | — | 1 | 6.89 |
| CHEMBL5203743 | — | — | 1 | 6.60 |
| CHEMBL5183834 | — | — | 1 | 6.37 |
| CHEMBL5182926 | — | — | 1 | 5.97 |
| CHEMBL5179622 | — | — | 1 | 5.57 |
| CHEMBL5171358 | — | — | 1 | 5.37 |
| CHEMBL5179345 | — | — | 1 | 4.76 |
| CHEMBL5183117 | — | — | 1 | - |
| CHEMBL5199496 | — | — | 1 | - |
| CHEMBL5203131 | — | — | 1 | - |
| CHEMBL5184465 | — | — | 1 | - |
| CHEMBL5174137 | — | — | 1 | - |
| CHEMBL5201451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397237 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5195797 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5173775 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5186932 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5203743 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5183834 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5182926 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL5179622 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL5171358 | — | IC50 | = | 4260.0 | nM | 5.37 |
| CHEMBL5179345 | — | IC50 | = | 17170.0 | nM | 4.76 |
| CHEMBL5183117 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5199496 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5203131 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5184465 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5174137 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5201451 | — | IC50 | > | 30000.0 | nM | - |