Assay Detail
Binding
CHEMBL4122879
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Inhibition of recombinant human renin using angiotensinogen as substrate pretreated for 10 mins followed by substrate addition measured after 30 mins in presence of human serum albumin by ELISA
24
Total Activities
24
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 benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.77 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4130200 | — | — | 1 | 9.49 |
| CHEMBL3958809 | — | — | 1 | 9.42 |
| CHEMBL4125900 | — | — | 1 | 9.23 |
| CHEMBL4126136 | — | — | 1 | 9.19 |
| CHEMBL4129081 | — | — | 1 | 9.19 |
| CHEMBL4127179 | — | — | 1 | 9.18 |
| CHEMBL4129207 | — | — | 1 | 9.09 |
| CHEMBL3990145 | IMARIKIREN | 2.0 | 1 | 9.08 |
| CHEMBL4129865 | — | — | 1 | 9.05 |
| CHEMBL4130109 | — | — | 1 | 8.96 |
| CHEMBL4127686 | — | — | 1 | 8.92 |
| CHEMBL4128929 | — | — | 1 | 8.85 |
| CHEMBL4128795 | — | — | 1 | 8.82 |
| CHEMBL4128438 | — | — | 1 | 8.80 |
| CHEMBL4126453 | — | — | 1 | 8.74 |
| CHEMBL4127842 | — | — | 1 | 8.68 |
| CHEMBL4126609 | — | — | 1 | 8.57 |
| CHEMBL4129831 | — | — | 1 | 8.48 |
| CHEMBL4129724 | — | — | 1 | 8.44 |
| CHEMBL4126759 | — | — | 1 | 7.68 |
| CHEMBL3889771 | — | — | 1 | 7.62 |
| CHEMBL4126556 | — | — | 1 | 7.46 |
| CHEMBL4127516 | — | — | 1 | - |
| CHEMBL4128342 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4130200 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL3958809 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4125900 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4126136 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL4129081 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4127179 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4129207 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL3990145 | IMARIKIREN | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL4129865 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4130109 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4127686 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4128929 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4128795 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4128438 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4126453 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4127842 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4126609 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4129831 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4129724 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4126759 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3889771 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4126556 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4127516 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4128342 | — | IC50 | > | 100.0 | nM | - |