Assay Detail
Binding
CHEMBL4774281
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR2 (unknown origin) expressed in U2OS cells cotransfected with beta-arrestin/TEV protease fusion protein and beta-lactamase assessed as inhibition of CXCL8-induced beta arrestin2 recruitment preincubated for 30 mins followed by CXCL8 stimulation and measured after 5 hrs by FRET based fluorescence/Tango assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 5.50 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38182 | — | — | 1 | 6.82 |
| CHEMBL4776480 | — | — | 1 | 5.96 |
| CHEMBL4787874 | — | — | 1 | 5.80 |
| CHEMBL4798569 | — | — | 1 | 5.80 |
| CHEMBL4795943 | — | — | 1 | 5.77 |
| CHEMBL4777868 | — | — | 1 | 5.75 |
| CHEMBL4787966 | — | — | 1 | 5.72 |
| CHEMBL4791845 | — | — | 1 | 5.70 |
| CHEMBL4793810 | — | — | 1 | 5.68 |
| CHEMBL4790233 | — | — | 1 | 5.66 |
| CHEMBL4788391 | — | — | 1 | 5.64 |
| CHEMBL4794294 | — | — | 1 | 5.62 |
| CHEMBL4786878 | — | — | 1 | 5.60 |
| CHEMBL4794114 | — | — | 1 | 5.60 |
| CHEMBL4787532 | — | — | 1 | 5.57 |
| CHEMBL4782078 | — | — | 1 | 5.57 |
| CHEMBL4782371 | — | — | 1 | 5.57 |
| CHEMBL4793669 | — | — | 1 | 5.52 |
| CHEMBL4784641 | — | — | 1 | 5.47 |
| CHEMBL4780042 | — | — | 1 | 5.41 |
| CHEMBL4792599 | — | — | 1 | 5.39 |
| CHEMBL4798282 | — | — | 1 | 5.36 |
| CHEMBL4779981 | — | — | 1 | 5.24 |
| CHEMBL4781097 | — | — | 1 | 5.19 |
| CHEMBL4780140 | — | — | 1 | 5.17 |
| CHEMBL4778886 | — | — | 1 | 5.17 |
| CHEMBL4788608 | — | — | 1 | 5.17 |
| CHEMBL4795585 | — | — | 1 | 5.16 |
| CHEMBL4782034 | — | — | 1 | 5.12 |
| CHEMBL4779885 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38182 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4776480 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4798569 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4787874 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4795943 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4777868 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4787966 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4791845 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4793810 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4790233 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4788391 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4794294 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4794114 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4786878 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4782371 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4787532 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4782078 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4793669 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4784641 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4780042 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4792599 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4798282 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4779981 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4781097 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4778886 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4788608 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4780140 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4795585 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4782034 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4779885 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4798148 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4796430 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4800160 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4794006 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4788927 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4796058 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4800238 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4786254 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4781241 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4785912 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4799102 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4777482 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4787491 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4787028 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4777007 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4792945 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4780039 | — | IC50 | > | 10000.0 | nM | - |