Assay Detail
Functional
CHEMBL4715191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 1,5-Dihydro-4H-imidazol-4-one Derivatives as Potent, Selective Antagonists of CXC Chemokine Receptor 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.50 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4786074 | — | — | 1 | 8.22 |
| CHEMBL4763312 | — | — | 1 | 8.05 |
| CHEMBL4742368 | — | — | 1 | 8.00 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | 2.0 | 1 | 8.00 |
| CHEMBL4757674 | — | — | 1 | 7.82 |
| CHEMBL4746698 | — | — | 1 | 7.54 |
| CHEMBL4747035 | — | — | 1 | 7.37 |
| CHEMBL4752486 | — | — | 1 | 7.27 |
| CHEMBL4793352 | — | — | 1 | 7.17 |
| CHEMBL4741864 | — | — | 1 | 7.01 |
| CHEMBL4750465 | — | — | 1 | 6.85 |
| CHEMBL4800297 | — | — | 1 | 6.57 |
| CHEMBL4746803 | — | — | 1 | 6.52 |
| CHEMBL4799848 | — | — | 1 | 6.52 |
| CHEMBL4786309 | — | — | 1 | 6.33 |
| CHEMBL4757462 | — | — | 1 | 6.04 |
| CHEMBL4797191 | — | — | 1 | 5.66 |
| CHEMBL4755486 | — | — | 1 | 5.55 |
| CHEMBL4762597 | — | — | 1 | 5.51 |
| CHEMBL4745933 | — | — | 1 | 5.40 |
| CHEMBL4536494 | — | — | 1 | 4.82 |
| CHEMBL4777637 | — | — | 1 | 4.63 |
| CHEMBL4760919 | — | — | 1 | 4.60 |
| CHEMBL4765070 | — | — | 1 | 4.53 |
| CHEMBL4797342 | — | — | 1 | - |
| CHEMBL4781979 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4786074 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4763312 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4742368 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL216981 | NAVARIXIN ANHYDROUS | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4757674 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4746698 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4747035 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4752486 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4793352 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4741864 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4750465 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4800297 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4746803 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4799848 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4786309 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4757462 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL4797191 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL4755486 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4762597 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4745933 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4536494 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4777637 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4760919 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4765070 | — | IC50 | = | 29700.0 | nM | 4.53 |
| CHEMBL4797342 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4781979 | — | IC50 | > | 100000.0 | nM | - |