Assay Detail
Functional
CHEMBL4407127
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Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.96 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4551932 | — | — | 1 | 9.09 |
| CHEMBL4462511 | — | — | 1 | 9.05 |
| CHEMBL4457190 | — | — | 1 | 9.01 |
| CHEMBL3728724 | — | — | 1 | 9.00 |
| CHEMBL4457819 | — | — | 1 | 8.96 |
| CHEMBL3728462 | — | — | 1 | 8.92 |
| CHEMBL4461217 | — | — | 1 | 8.92 |
| CHEMBL4447049 | — | — | 1 | 8.89 |
| CHEMBL4452111 | — | — | 1 | 8.80 |
| CHEMBL4539616 | — | — | 1 | 8.80 |
| CHEMBL4580391 | — | — | 1 | 8.74 |
| CHEMBL4537548 | — | — | 1 | 8.64 |
| CHEMBL3728620 | — | — | 1 | 8.62 |
| CHEMBL4441723 | — | — | 1 | 8.62 |
| CHEMBL3732386 | — | — | 1 | 8.55 |
| CHEMBL4523001 | — | — | 1 | 8.51 |
| CHEMBL4483493 | — | — | 1 | 8.51 |
| CHEMBL4465125 | — | — | 1 | 8.49 |
| CHEMBL4528562 | — | — | 1 | 8.49 |
| CHEMBL4474285 | — | — | 1 | 8.48 |
| CHEMBL4476101 | — | — | 1 | 8.47 |
| CHEMBL3931873 | — | — | 1 | 8.40 |
| CHEMBL3732490 | — | — | 1 | 8.38 |
| CHEMBL4452516 | — | — | 1 | 8.37 |
| CHEMBL4439280 | — | — | 1 | 8.12 |
| CHEMBL4459685 | — | — | 1 | 8.03 |
| CHEMBL3727598 | — | — | 1 | 7.96 |
| CHEMBL3728507 | — | — | 1 | 7.96 |
| CHEMBL4454407 | — | — | 1 | 7.96 |
| CHEMBL4445561 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4551932 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4462511 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4457190 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3728724 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL4457819 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3728462 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4461217 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4447049 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4452111 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4539616 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4580391 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4537548 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3728620 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4441723 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3732386 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4523001 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4483493 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4465125 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4528562 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4474285 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4476101 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3931873 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3732490 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4452516 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4439280 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4459685 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3727598 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3728507 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4454407 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4445561 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3730957 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3731720 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4529377 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3728010 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3729282 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3732510 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3730643 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3731871 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3728130 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4572935 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4471641 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3732594 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4435447 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4444227 | — | IC50 | = | 2900.0 | nM | 5.54 |