Assay Detail
Binding
CHEMBL4037528
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR2 in human whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 15 mins followed by GROalpha stimulation measured after 15 mins by FITC-staining based FACS analysis
35
Total Activities
34
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 Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.66 | 7.40 |
| pIC50 | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4067429 | — | — | 2 | 7.40 |
| CHEMBL4098864 | — | — | 1 | 7.20 |
| CHEMBL4076428 | — | — | 1 | 7.00 |
| CHEMBL4079102 | — | — | 1 | 7.00 |
| CHEMBL4097602 | — | — | 1 | 6.90 |
| CHEMBL4062546 | — | — | 1 | 6.90 |
| CHEMBL4082136 | — | — | 1 | 6.80 |
| CHEMBL4100674 | — | — | 1 | 6.80 |
| CHEMBL4098979 | — | — | 1 | 6.70 |
| CHEMBL4060060 | — | — | 1 | 6.70 |
| CHEMBL4066510 | — | — | 1 | 6.70 |
| CHEMBL4079718 | — | — | 1 | 6.60 |
| CHEMBL4081963 | — | — | 1 | 6.60 |
| CHEMBL4084135 | — | — | 1 | 6.50 |
| CHEMBL4095602 | — | — | 1 | 6.50 |
| CHEMBL4084077 | — | — | 1 | 6.40 |
| CHEMBL4088551 | — | — | 1 | 6.40 |
| CHEMBL4077201 | — | — | 1 | 6.40 |
| CHEMBL4070506 | — | — | 1 | 6.30 |
| CHEMBL4072010 | — | — | 1 | 6.20 |
| CHEMBL4086957 | — | — | 1 | 6.20 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 6.17 |
| CHEMBL4066904 | — | — | 1 | 6.00 |
| CHEMBL4089421 | — | — | 1 | - |
| CHEMBL4062361 | — | — | 1 | - |
| CHEMBL4072270 | — | — | 1 | - |
| CHEMBL4076053 | — | — | 1 | - |
| CHEMBL4076478 | — | — | 1 | - |
| CHEMBL4103349 | — | — | 1 | - |
| CHEMBL4065522 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4067429 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4067429 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4098864 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4076428 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4079102 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4097602 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4062546 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4082136 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4100674 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4098979 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4066510 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4060060 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4079718 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4081963 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4095602 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4084135 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4077201 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4084077 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4088551 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4070506 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4072010 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4086957 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4066904 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4076053 | — | pIC50 | - | — | - | |
| CHEMBL4072270 | — | pIC50 | - | — | - | |
| CHEMBL4089421 | — | pIC50 | - | — | - | |
| CHEMBL4070629 | — | pIC50 | - | — | - | |
| CHEMBL4092148 | — | pIC50 | - | — | - | |
| CHEMBL4060778 | — | pIC50 | - | — | - | |
| CHEMBL4065522 | — | pIC50 | - | — | - | |
| CHEMBL4103349 | — | pIC50 | - | — | - | |
| CHEMBL4076676 | — | pIC50 | - | — | - | |
| CHEMBL4076478 | — | pIC50 | - | — | - | |
| CHEMBL4062361 | — | pIC50 | - | — | - |