Assay Detail
Functional
CHEMBL4123964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isoxazole-tethered diarylheptanoid analogs: Discovery of a new drug-like PAR2 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 5.28 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127372 | — | — | 1 | 5.38 |
| CHEMBL4128763 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127372 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4128763 | — | IC50 | = | 6600.0 | nM | 5.18 |