Assay Detail
Functional
CHEMBL690699
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Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by endothelial NOS (e NOS) from HUVEC cells
24
Total Activities
24
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
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.06 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7945 | — | — | 1 | 6.80 |
| CHEMBL256147 | TILARGININE | 3.0 | 1 | 6.52 |
| CHEMBL8272 | — | — | 1 | 6.05 |
| CHEMBL7891 | — | — | 1 | 5.70 |
| CHEMBL7889 | L-NIL | — | 1 | 5.62 |
| CHEMBL7890 | L-NAME | 2.0 | 1 | 5.57 |
| CHEMBL7931 | — | — | 1 | 5.44 |
| CHEMBL8390 | — | — | 1 | 5.40 |
| CHEMBL266226 | — | — | 1 | 5.30 |
| CHEMBL267075 | — | — | 1 | 5.30 |
| CHEMBL7934 | — | — | 1 | 5.22 |
| CHEMBL8065 | — | — | 1 | 5.10 |
| CHEMBL440270 | — | — | 1 | 5.05 |
| CHEMBL273659 | — | — | 1 | 5.05 |
| CHEMBL268668 | — | — | 1 | 4.92 |
| CHEMBL274402 | — | — | 1 | 4.72 |
| CHEMBL8088 | — | — | 1 | 4.40 |
| CHEMBL7969 | — | — | 1 | 4.36 |
| CHEMBL268403 | — | — | 1 | 4.36 |
| CHEMBL275955 | — | — | 1 | 4.26 |
| CHEMBL225304 | PIMAGEDINE | 2.0 | 1 | 4.14 |
| CHEMBL414608 | — | — | 1 | 4.10 |
| CHEMBL7873 | — | — | 1 | 4.07 |
| CHEMBL7946 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7945 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL256147 | TILARGININE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL8272 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL7891 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL7889 | L-NIL | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL7890 | L-NAME | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL7931 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL8390 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL266226 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL267075 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL7934 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL8065 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL440270 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL273659 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL268668 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL274402 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL8088 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL7969 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL268403 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL275955 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL225304 | PIMAGEDINE | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL414608 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL7873 | — | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL7946 | — | IC50 | = | 100000.0 | nM | 4.00 |