Assay Detail
Binding
CHEMBL5149787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant renin using Nma-Lys-His-Pro-Phe-His-Leu-Val-Ile-His-Lys-Dnp substrate incubated for 1 hr by FRET
23
Total Activities
23
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
Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.75 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1639 | ALISKIREN | 4.0 | 1 | 9.15 |
| CHEMBL5187830 | — | — | 1 | 9.05 |
| CHEMBL5203297 | — | — | 1 | 8.85 |
| CHEMBL5186584 | — | — | 1 | 8.37 |
| CHEMBL5176733 | — | — | 1 | 8.24 |
| CHEMBL5174842 | — | — | 1 | 8.03 |
| CHEMBL5170164 | — | — | 1 | 8.00 |
| CHEMBL3699637 | — | — | 1 | 7.89 |
| CHEMBL5197721 | — | — | 1 | 7.72 |
| CHEMBL5203591 | — | — | 1 | 7.64 |
| CHEMBL3699636 | — | — | 1 | 7.52 |
| CHEMBL5188797 | — | — | 1 | 6.99 |
| CHEMBL5183309 | — | — | 1 | 6.93 |
| CHEMBL5206846 | — | — | 1 | 6.80 |
| CHEMBL5185167 | — | — | 1 | 6.56 |
| CHEMBL5181888 | — | — | 1 | 6.23 |
| CHEMBL5205574 | — | — | 1 | - |
| CHEMBL5176378 | — | — | 1 | - |
| CHEMBL5187637 | — | — | 1 | - |
| CHEMBL5177567 | — | — | 1 | - |
| CHEMBL5186347 | — | — | 1 | - |
| CHEMBL5199179 | — | — | 1 | - |
| CHEMBL5185263 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1639 | ALISKIREN | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5187830 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5203297 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5186584 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5176733 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5174842 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5170164 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3699637 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5197721 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5203591 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3699636 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5188797 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5183309 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL5206846 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5185167 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL5181888 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL5205574 | — | IC50 | - | — | - | |
| CHEMBL5176378 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5187637 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5177567 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5186347 | — | IC50 | - | — | - | |
| CHEMBL5199179 | — | IC50 | - | — | - | |
| CHEMBL5185263 | — | IC50 | - | — | - |