Assay Detail
Binding
CHEMBL963305
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Binding affinity to CXCR2
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.14 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523769 | — | — | 1 | 8.70 |
| CHEMBL473959 | — | — | 1 | 8.70 |
| CHEMBL254370 | — | — | 1 | 8.40 |
| CHEMBL516184 | — | — | 1 | 8.40 |
| CHEMBL523645 | — | — | 1 | 8.40 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 8.40 |
| CHEMBL473145 | — | — | 1 | 8.30 |
| CHEMBL515262 | — | — | 1 | 8.30 |
| CHEMBL523807 | — | — | 1 | 8.30 |
| CHEMBL491135 | — | — | 1 | 8.30 |
| CHEMBL518857 | — | — | 1 | 8.30 |
| CHEMBL523437 | — | — | 1 | 8.30 |
| CHEMBL491134 | — | — | 1 | 8.15 |
| CHEMBL472749 | — | — | 1 | 8.15 |
| CHEMBL491487 | — | — | 1 | 8.10 |
| CHEMBL491312 | — | — | 1 | 8.05 |
| CHEMBL491330 | — | — | 1 | 8.00 |
| CHEMBL491506 | — | — | 1 | 7.92 |
| CHEMBL514001 | — | — | 1 | 7.89 |
| CHEMBL523984 | — | — | 1 | 7.85 |
| CHEMBL464301 | — | — | 1 | 7.85 |
| CHEMBL473561 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523769 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL473959 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL254370 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL516184 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL523645 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL473145 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL515262 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL523807 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL491135 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL518857 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL523437 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL491134 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL472749 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL491487 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL491312 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL491330 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL491506 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL514001 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL523984 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL464301 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL473561 | — | Ki | = | 400.0 | nM | 6.40 |