Assay Detail
Functional
CHEMBL665580
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Ability to inhibit the conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by i-NOS from human DLD-1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | DLD-1 |
| 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 | 16 | 6.20 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8292 | — | — | 1 | 7.40 |
| CHEMBL8365 | — | — | 1 | 7.29 |
| CHEMBL274405 | — | — | 1 | 7.05 |
| CHEMBL8281 | — | — | 1 | 6.96 |
| CHEMBL8041 | — | — | 1 | 6.82 |
| CHEMBL8302 | — | — | 1 | 6.82 |
| CHEMBL8105 | — | — | 1 | 6.72 |
| CHEMBL256147 | TILARGININE | 3.0 | 1 | 6.52 |
| CHEMBL268521 | — | — | 1 | 6.14 |
| CHEMBL274207 | — | — | 1 | 5.80 |
| CHEMBL416696 | — | — | 1 | 5.57 |
| CHEMBL412901 | — | — | 1 | 5.55 |
| CHEMBL8304 | — | — | 1 | 5.46 |
| CHEMBL8288 | — | — | 1 | 5.44 |
| CHEMBL8106 | — | — | 1 | 5.08 |
| CHEMBL269162 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8292 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL8365 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL274405 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL8281 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL8041 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL8302 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL8105 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL256147 | TILARGININE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL268521 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL274207 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL416696 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL412901 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL8304 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL8288 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL8106 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL269162 | — | IC50 | = | 28000.0 | nM | 4.55 |