Assay Detail
Binding
CHEMBL2421978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of trypsin-activated human recombinant renin using (Arg-Glu(EDANS)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(DABCYL)-Arg) as substrate incubated for 10 mins prior to substrate addition measured after 90 mins by fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.72 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2419040 | — | — | 1 | 9.00 |
| CHEMBL2419042 | — | — | 1 | 8.96 |
| CHEMBL2419045 | — | — | 1 | 8.89 |
| CHEMBL2204732 | — | — | 1 | 8.89 |
| CHEMBL2419046 | — | — | 1 | 8.85 |
| CHEMBL2419044 | — | — | 1 | 8.80 |
| CHEMBL2204739 | — | — | 1 | 8.80 |
| CHEMBL2419041 | — | — | 1 | 8.77 |
| CHEMBL2419048 | — | — | 1 | 8.74 |
| CHEMBL2419043 | — | — | 1 | 8.72 |
| CHEMBL2204734 | — | — | 1 | 8.68 |
| CHEMBL2204740 | — | — | 1 | 8.68 |
| CHEMBL2204017 | — | — | 1 | 8.68 |
| CHEMBL2419050 | — | — | 1 | 8.64 |
| CHEMBL2204018 | — | — | 1 | 8.64 |
| CHEMBL2419049 | — | — | 1 | 8.62 |
| CHEMBL2204741 | — | — | 1 | 8.60 |
| CHEMBL2419047 | — | — | 1 | 8.48 |
| CHEMBL2419039 | — | — | 1 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2419040 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2419042 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2419045 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2204732 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2419046 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2419044 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2204739 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2419041 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2419048 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2419043 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2204734 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2204740 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2204017 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2419050 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2204018 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2419049 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2204741 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2419047 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2419039 | — | IC50 | = | 5.2 | nM | 8.28 |