Assay Detail
Functional
CHEMBL4628495
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
6
Total Activities
6
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
Design and synthesis of potent PAR-1 antagonists based on vorapaxar.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.32 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639789 | — | — | 1 | 6.75 |
| CHEMBL493982 | VORAPAXAR | 4.0 | 1 | 6.60 |
| CHEMBL4632907 | — | — | 1 | 6.26 |
| CHEMBL4633888 | — | — | 1 | 6.21 |
| CHEMBL4639680 | — | — | 1 | 6.12 |
| CHEMBL4633243 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639789 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL493982 | VORAPAXAR | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4632907 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4633888 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4639680 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4633243 | — | IC50 | = | 1100.0 | nM | 5.96 |