Assay Detail
Functional
CHEMBL927480
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR1/CXCR2 in human PMN cells assessed as inhibition of GROalpha-mediated myeloperoxidase release
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PMN |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Interleukin-8 receptors, CXCR1/CXCR2 (CHEMBL2096909) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.43 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403547 | — | — | 1 | 8.10 |
| CHEMBL254942 | — | — | 1 | 8.10 |
| CHEMBL254943 | — | — | 1 | 7.89 |
| CHEMBL403206 | — | — | 1 | 7.57 |
| CHEMBL253305 | — | — | 1 | 7.55 |
| CHEMBL403936 | — | — | 1 | 7.42 |
| CHEMBL252911 | — | — | 1 | 6.88 |
| CHEMBL253306 | — | — | 1 | 6.88 |
| CHEMBL253304 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403547 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL254942 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL254943 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL403206 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL253305 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL403936 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL252911 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL253306 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL253304 | — | IC50 | = | 331.0 | nM | 6.48 |