Assay Detail
Functional
CHEMBL4311920
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Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| 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 |
|---|---|---|---|
| IC50 | 3 | 7.72 | 8.30 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7642 | RWJ-58259 | — | 1 | 8.30 |
| CHEMBL4459024 | — | — | 1 | 8.00 |
| CHEMBL4540591 | — | — | 1 | 6.85 |
| CHEMBL4532248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7642 | RWJ-58259 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4459024 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4540591 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4532248 | — | Inhibition | - | % | - |