Assay Detail
Binding
CHEMBL1799738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of renin in human plasma using Q-FRET substrate pretreated for 10 mins before substrate addition measured after 1 hr
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.15 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1796075 | — | — | 1 | 9.32 |
| CHEMBL1796078 | — | — | 1 | 9.28 |
| CHEMBL1796071 | — | — | 1 | 9.24 |
| CHEMBL1796073 | — | — | 1 | 9.21 |
| CHEMBL1796074 | — | — | 1 | 9.20 |
| CHEMBL1796070 | — | — | 1 | 9.19 |
| CHEMBL1796069 | — | — | 1 | 9.06 |
| CHEMBL1796061 | — | — | 1 | 9.00 |
| CHEMBL1795909 | — | — | 1 | 8.89 |
| CHEMBL1796065 | — | — | 1 | 8.85 |
| CHEMBL1796077 | — | — | 1 | 8.70 |
| CHEMBL1795912 | — | — | 1 | 8.66 |
| CHEMBL1796067 | — | — | 1 | 8.66 |
| CHEMBL1796063 | — | — | 1 | 8.62 |
| CHEMBL1796066 | — | — | 1 | 8.52 |
| CHEMBL1796062 | — | — | 1 | 8.46 |
| CHEMBL1761519 | — | — | 1 | 8.30 |
| CHEMBL1796068 | — | — | 1 | 8.28 |
| CHEMBL1795911 | — | — | 1 | 8.19 |
| CHEMBL1795907 | — | — | 1 | 8.10 |
| CHEMBL1796072 | — | — | 1 | 8.08 |
| CHEMBL1795915 | — | — | 1 | 8.05 |
| CHEMBL1795913 | — | — | 1 | 8.00 |
| CHEMBL1795914 | — | — | 1 | 7.77 |
| CHEMBL1795910 | — | — | 1 | 7.60 |
| CHEMBL1796060 | — | — | 1 | 7.58 |
| CHEMBL1795903 | — | — | 1 | 7.51 |
| CHEMBL1795906 | — | — | 1 | 7.41 |
| CHEMBL1795908 | — | — | 1 | 7.38 |
| CHEMBL1795905 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1796075 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL1796078 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL1796071 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL1796073 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL1796074 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL1796070 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL1796069 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL1796061 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1795909 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1796065 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1796077 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1795912 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1796067 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1796063 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1796066 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1796062 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1761519 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1796068 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL1795911 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1795907 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1796072 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1795915 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1795913 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1795914 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1795910 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1796060 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1795903 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1795906 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1795908 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1795905 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1796064 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1795902 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1795916 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1795904 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1795901 | — | IC50 | = | 580.0 | nM | 6.24 |