Assay Detail
Functional
CHEMBL996091
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Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and selective small-molecule PAR-2 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 6.32 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459723 | — | — | 1 | 7.60 |
| CHEMBL509819 | — | — | 1 | 7.60 |
| CHEMBL494502 | — | — | 3 | 7.50 |
| CHEMBL461639 | — | — | 1 | 7.30 |
| CHEMBL459509 | — | — | 1 | 6.90 |
| CHEMBL493076 | — | — | 1 | 6.70 |
| CHEMBL493704 | — | — | 1 | 5.60 |
| CHEMBL459724 | — | — | 1 | 5.20 |
| CHEMBL494303 | — | — | 1 | 5.20 |
| CHEMBL494503 | — | — | 1 | 5.10 |
| CHEMBL238078 | — | — | 1 | 5.00 |
| CHEMBL493494 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459723 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL509819 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL494502 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL494502 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL461639 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL459509 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL493076 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL493704 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL459724 | — | EC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL494303 | — | EC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL494503 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL238078 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL493494 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL494502 | — | EC50 | > | 10000.0 | nM | - |