Assay Detail
Binding
CHEMBL5366015
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Binding affinity to NanoLuc fused Snap CXCR2 (unknown origin) expressed in HEK293 cell membrane assessed as inhibition constant using furimazine as substrate incubated with substrate for 5 mins and measured every 15 secs for 60 mins by luminescence based NanoBRET fluorescent binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.50 | 9.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4562140 | — | — | 1 | 9.61 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 9.19 |
| CHEMBL5421394 | — | — | 1 | 8.87 |
| CHEMBL3039531 | DANIRIXIN | 2.0 | 1 | 8.71 |
| CHEMBL38182 | — | — | 1 | 8.68 |
| CHEMBL218964 | — | — | 1 | 8.48 |
| CHEMBL403225 | — | — | 1 | 8.32 |
| CHEMBL5424054 | — | — | 1 | 8.31 |
| CHEMBL5404638 | — | — | 1 | 8.16 |
| CHEMBL1162935 | — | — | 1 | 8.06 |
| CHEMBL5398802 | — | — | 1 | 7.97 |
| CHEMBL5423846 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4562140 | — | Ki | = | 0.2455 | nM | 9.61 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | Ki | = | 0.6457 | nM | 9.19 |
| CHEMBL5421394 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL3039531 | DANIRIXIN | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL38182 | — | Ki | = | 2.089 | nM | 8.68 |
| CHEMBL218964 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL403225 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL5424054 | — | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL5404638 | — | Ki | = | 6.918 | nM | 8.16 |
| CHEMBL1162935 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL5398802 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL5423846 | — | Ki | = | 23.99 | nM | 7.62 |