Assay Detail
Binding
CHEMBL3821596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
29
Total Activities
29
Compounds Tested
1
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 | 29 | 9.08 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3818853 | — | — | 1 | 9.50 |
| CHEMBL3818984 | — | — | 1 | 9.50 |
| CHEMBL3819480 | — | — | 1 | 9.50 |
| CHEMBL3818581 | — | — | 1 | 9.40 |
| CHEMBL3819163 | — | — | 1 | 9.40 |
| CHEMBL3819221 | — | — | 1 | 9.30 |
| CHEMBL3818827 | — | — | 1 | 9.30 |
| CHEMBL3818277 | — | — | 1 | 9.30 |
| CHEMBL3819512 | — | — | 1 | 9.30 |
| CHEMBL3818793 | — | — | 1 | 9.30 |
| CHEMBL3819569 | — | — | 1 | 9.30 |
| CHEMBL3817901 | — | — | 1 | 9.30 |
| CHEMBL3819295 | — | — | 1 | 9.30 |
| CHEMBL3818216 | — | — | 1 | 9.20 |
| CHEMBL3818458 | — | — | 1 | 9.20 |
| CHEMBL3818820 | — | — | 1 | 9.10 |
| CHEMBL3819542 | — | — | 1 | 9.10 |
| CHEMBL3818917 | — | — | 1 | 9.10 |
| CHEMBL3818323 | — | — | 1 | 9.00 |
| CHEMBL3819382 | — | — | 1 | 9.00 |
| CHEMBL3818331 | — | — | 1 | 8.90 |
| CHEMBL3818179 | — | — | 1 | 8.90 |
| CHEMBL3819603 | — | — | 1 | 8.80 |
| CHEMBL3819521 | — | — | 1 | 8.80 |
| CHEMBL3818269 | — | — | 1 | 8.70 |
| CHEMBL3819070 | — | — | 1 | 8.70 |
| CHEMBL3819292 | — | — | 1 | 8.70 |
| CHEMBL3819013 | — | — | 1 | 8.40 |
| CHEMBL3817880 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3818853 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3818984 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3819480 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3818581 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL3819163 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL3819221 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3818827 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3818277 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3819512 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3818793 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3819569 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3817901 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3819295 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3818216 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL3818458 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL3818820 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3819542 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3818917 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3818323 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3819382 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3818331 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL3818179 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL3819603 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL3819521 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL3818269 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL3819070 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL3819292 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL3819013 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3817880 | — | IC50 | = | 10.0 | nM | 8.00 |