Assay Detail
Binding
CHEMBL817560
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.80 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304924 | — | — | 1 | 6.62 |
| CHEMBL63966 | — | — | 1 | 6.52 |
| CHEMBL431369 | — | — | 1 | 6.42 |
| CHEMBL438551 | — | — | 1 | 6.36 |
| CHEMBL67308 | — | — | 1 | 6.30 |
| CHEMBL433499 | — | — | 1 | 6.14 |
| CHEMBL265227 | — | — | 1 | 6.10 |
| CHEMBL428311 | — | — | 1 | 6.09 |
| CHEMBL304128 | — | — | 1 | 6.04 |
| CHEMBL62775 | — | — | 1 | 6.00 |
| CHEMBL304120 | — | — | 1 | 5.96 |
| CHEMBL7610 | RWJ-54003 | — | 1 | 5.89 |
| CHEMBL304827 | — | — | 1 | 5.89 |
| CHEMBL293867 | — | — | 1 | 5.89 |
| CHEMBL302433 | — | — | 1 | 5.75 |
| CHEMBL269345 | — | — | 1 | 5.66 |
| CHEMBL303157 | — | — | 1 | 5.64 |
| CHEMBL303187 | — | — | 1 | 5.60 |
| CHEMBL62584 | — | — | 1 | 5.60 |
| CHEMBL65004 | — | — | 1 | 5.58 |
| CHEMBL63402 | — | — | 1 | 5.58 |
| CHEMBL68458 | — | — | 1 | 5.51 |
| CHEMBL304829 | — | — | 1 | 5.50 |
| CHEMBL66958 | — | — | 1 | 5.48 |
| CHEMBL302823 | — | — | 1 | 5.46 |
| CHEMBL304683 | — | — | 1 | 5.28 |
| CHEMBL302603 | — | — | 1 | 5.25 |
| CHEMBL66585 | — | — | 1 | 5.19 |
| CHEMBL305188 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304924 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL63966 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL431369 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL438551 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL67308 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL433499 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL265227 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL428311 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL304128 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL62775 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL304120 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL7610 | RWJ-54003 | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL304827 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL293867 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL302433 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL269345 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL303157 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL303187 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL62584 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL65004 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL63402 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL68458 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL304829 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL66958 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL302823 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL304683 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL302603 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL66585 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL305188 | — | IC50 | = | 11200.0 | nM | 4.95 |