Assay Detail
Functional
CHEMBL693033
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Ability to inhibit the conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by e-NOS from HUVEC cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HUVEC |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.08 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8365 | — | — | 1 | 7.30 |
| CHEMBL8292 | — | — | 1 | 7.10 |
| CHEMBL8281 | — | — | 1 | 6.92 |
| CHEMBL268521 | — | — | 1 | 6.55 |
| CHEMBL256147 | TILARGININE | 3.0 | 1 | 6.52 |
| CHEMBL8105 | — | — | 1 | 6.12 |
| CHEMBL274405 | — | — | 1 | 6.04 |
| CHEMBL8041 | — | — | 1 | 5.72 |
| CHEMBL8106 | — | — | 1 | 5.40 |
| CHEMBL8302 | — | — | 1 | 5.30 |
| CHEMBL416696 | — | — | 1 | 5.02 |
| CHEMBL8304 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8365 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL8292 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL8281 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL268521 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL256147 | TILARGININE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL8105 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL274405 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL8041 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL8106 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL8302 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL416696 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL8304 | — | IC50 | = | 10000.0 | nM | 5.00 |