Assay Detail
Binding
CHEMBL3390699
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Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.26 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3334887 | — | — | 1 | 7.18 |
| CHEMBL125021 | — | — | 1 | 6.89 |
| CHEMBL1609104 | — | — | 1 | 6.85 |
| CHEMBL3334944 | — | — | 1 | 6.55 |
| CHEMBL3334941 | — | — | 1 | 6.47 |
| CHEMBL3334940 | — | — | 1 | 6.19 |
| CHEMBL3334939 | — | — | 1 | 6.11 |
| CHEMBL3334942 | — | — | 1 | 6.10 |
| CHEMBL3334943 | — | — | 1 | 5.29 |
| CHEMBL3334933 | — | — | 1 | 5.00 |
| CHEMBL3334901 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3334887 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL125021 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1609104 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3334944 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL3334941 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL3334940 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL3334939 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL3334942 | — | IC50 | = | 793.0 | nM | 6.10 |
| CHEMBL3334943 | — | IC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL3334933 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3334901 | — | IC50 | > | 10000.0 | nM | - |