Assay Detail
Binding
CHEMBL862382
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Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 membranes by SPA
14
Total Activities
14
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
Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.20 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380732 | — | — | 1 | 8.02 |
| CHEMBL380947 | — | — | 1 | 7.85 |
| CHEMBL204552 | — | — | 1 | 7.30 |
| CHEMBL274737 | — | — | 1 | 6.92 |
| CHEMBL370387 | — | — | 1 | 6.57 |
| CHEMBL203715 | — | — | 1 | 6.46 |
| CHEMBL201842 | — | — | 1 | 6.32 |
| CHEMBL373067 | — | — | 1 | 5.89 |
| CHEMBL201204 | — | — | 1 | 5.85 |
| CHEMBL383235 | — | — | 1 | 5.41 |
| CHEMBL201921 | — | — | 1 | 5.16 |
| CHEMBL201800 | — | — | 1 | 5.00 |
| CHEMBL201672 | — | — | 1 | 5.00 |
| CHEMBL201799 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380732 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL380947 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL204552 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL274737 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL370387 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL203715 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL201842 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL373067 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL201204 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL383235 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL201921 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL201800 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL201672 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL201799 | — | IC50 | = | 10000.0 | nM | 5.00 |