Assay Detail
Binding
CHEMBL3821597
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant CXCR2 assessed as inhibition of CXCL1-induced neutrophil chemotaxis after 45 mins by calcein-AM dye based plate reader method
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.88 | 8.70 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3819070 | — | — | 1 | 8.70 |
| CHEMBL3819221 | — | — | 1 | 8.20 |
| CHEMBL3818820 | — | — | 1 | 8.20 |
| CHEMBL3818323 | — | — | 1 | 8.10 |
| CHEMBL3818793 | — | — | 1 | 8.10 |
| CHEMBL3817901 | — | — | 1 | 8.00 |
| CHEMBL3818984 | — | — | 1 | 7.90 |
| CHEMBL3818581 | — | — | 1 | 7.60 |
| CHEMBL3819512 | — | — | 1 | 7.60 |
| CHEMBL3818853 | — | — | 1 | 7.60 |
| CHEMBL3819569 | — | — | 1 | 7.40 |
| CHEMBL3819480 | — | — | 1 | 7.10 |
| CHEMBL3818277 | — | — | 1 | 7.10 |
| CHEMBL3818827 | — | — | 1 | 7.00 |
| CHEMBL3818216 | — | — | 1 | 6.80 |
| CHEMBL3818331 | — | — | 1 | 6.80 |
| CHEMBL3819521 | — | — | 1 | 6.80 |
| CHEMBL3818179 | — | — | 1 | 6.60 |
| CHEMBL3819292 | — | — | 1 | 6.50 |
| CHEMBL3818917 | — | — | 1 | 6.50 |
| CHEMBL3819163 | — | — | 1 | 6.20 |
| CHEMBL3819542 | — | — | 1 | 6.00 |
| CHEMBL3819603 | — | — | 1 | 5.70 |
| CHEMBL3819382 | — | — | 1 | 5.70 |
| CHEMBL3819013 | — | — | 1 | 5.50 |
| CHEMBL3819295 | — | — | 1 | 5.20 |
| CHEMBL3818458 | — | — | 1 | 5.00 |
| CHEMBL3817880 | — | — | 1 | 4.80 |
| CHEMBL3818269 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3819070 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL3819221 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3818820 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3818323 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3818793 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3817901 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3818984 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3818581 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3819512 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3818853 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3819569 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3819480 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3818277 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3818827 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3818216 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3818331 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3819521 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3818179 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3819292 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3818917 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3819163 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3819542 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3819603 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3819382 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3819013 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL3819295 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3818458 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3817880 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3818269 | — | pIC50 | - | — | - |