Assay Detail
Functional
CHEMBL4311925
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Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of trypsin-induced intracellular calcium mobilization preincubated for 15 mins followed by trypsin addition by Fluo-4-AM dye based fluorescence assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 2 | - | - |
| IC50 | 1 | 8.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470628 | — | — | 1 | 8.70 |
| CHEMBL4540591 | — | — | 1 | - |
| CHEMBL4588926 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470628 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4540591 | — | Inhibition | - | % | - | |
| CHEMBL4588926 | — | Inhibition | - | % | - |