Assay Detail
Functional
CHEMBL3583015
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Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibitors of the PAR-2 Signaling Pathway May Treat Pain and Inflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.56 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3582251 | — | — | 1 | 8.32 |
| CHEMBL3582250 | — | — | 1 | 8.30 |
| CHEMBL3582248 | — | — | 1 | 8.30 |
| CHEMBL3582249 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3582251 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3582250 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3582248 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3582249 | — | IC50 | = | 4800.0 | nM | 5.32 |