Assay Detail
Binding
CHEMBL4843847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Plasma |
| Cell Type | Platelet |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 74 | 5.61 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4860533 | — | — | 1 | 7.08 |
| CHEMBL4866566 | — | — | 1 | 6.96 |
| CHEMBL4849569 | — | — | 1 | 6.80 |
| CHEMBL4855875 | — | — | 1 | 6.77 |
| CHEMBL4855377 | — | — | 1 | 6.28 |
| CHEMBL4870185 | — | — | 1 | 6.19 |
| CHEMBL4857938 | — | — | 1 | 6.10 |
| CHEMBL4871001 | — | — | 1 | 6.08 |
| CHEMBL3728507 | — | — | 1 | 6.03 |
| CHEMBL4849478 | — | — | 1 | 6.02 |
| CHEMBL4866983 | — | — | 1 | 6.01 |
| CHEMBL4867779 | — | — | 1 | 6.00 |
| CHEMBL4871578 | — | — | 1 | 5.98 |
| CHEMBL4859532 | — | — | 1 | 5.91 |
| CHEMBL4849024 | — | — | 1 | 5.86 |
| CHEMBL4867321 | — | — | 1 | 5.86 |
| CHEMBL4871870 | — | — | 1 | 5.79 |
| CHEMBL4847592 | — | — | 1 | 5.74 |
| CHEMBL3728010 | — | — | 1 | 5.74 |
| CHEMBL4858844 | — | — | 1 | 5.73 |
| CHEMBL4864730 | — | — | 1 | 5.68 |
| CHEMBL4860348 | — | — | 1 | 5.68 |
| CHEMBL4865655 | — | — | 1 | 5.63 |
| CHEMBL4859012 | — | — | 1 | 5.60 |
| CHEMBL4862300 | — | — | 1 | 5.58 |
| CHEMBL4855122 | — | — | 1 | 5.58 |
| CHEMBL4849962 | — | — | 1 | 5.52 |
| CHEMBL4848044 | — | — | 1 | 5.52 |
| CHEMBL4855079 | — | — | 1 | 5.50 |
| CHEMBL4867000 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4860533 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4866566 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4849569 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4855875 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4855377 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4870185 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4857938 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4871001 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3728507 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4849478 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4866983 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4867779 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4871578 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4859532 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4867321 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4849024 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4871870 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4847592 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL3728010 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL4858844 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4864730 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL4860348 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL4865655 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4859012 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL4855122 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL4862300 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL4849962 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4848044 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4855079 | — | IC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL4867000 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL4849742 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL4866596 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL4874764 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL4873173 | — | IC50 | = | 3640.0 | nM | 5.44 |
| CHEMBL4847606 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4870259 | — | IC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL4877231 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4874590 | — | IC50 | = | 4260.0 | nM | 5.37 |
| CHEMBL4845780 | — | IC50 | = | 4260.0 | nM | 5.37 |
| CHEMBL4864292 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL4870778 | — | IC50 | = | 4820.0 | nM | 5.32 |
| CHEMBL4870833 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL4852886 | — | IC50 | = | 5480.0 | nM | 5.26 |
| CHEMBL4854301 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4866947 | — | IC50 | = | 5570.0 | nM | 5.25 |
| CHEMBL4863438 | — | IC50 | = | 6280.0 | nM | 5.20 |
| CHEMBL4858255 | — | IC50 | = | 6780.0 | nM | 5.17 |
| CHEMBL4860078 | — | IC50 | = | 6740.0 | nM | 5.17 |
| CHEMBL4877639 | — | IC50 | = | 7040.0 | nM | 5.15 |
| CHEMBL4876067 | — | IC50 | = | 7320.0 | nM | 5.13 |