Assay Detail
Binding
CHEMBL801709
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In vitro inhibitory activity against purified recombinant human renin
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.90 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31601 | REMIKIREN | 2.0 | 1 | 10.60 |
| CHEMBL430539 | — | — | 1 | 10.22 |
| CHEMBL417485 | — | — | 1 | 8.82 |
| CHEMBL31466 | — | — | 1 | 8.10 |
| CHEMBL285454 | — | — | 1 | 7.58 |
| CHEMBL431502 | — | — | 1 | 7.39 |
| CHEMBL283683 | — | — | 1 | 7.28 |
| CHEMBL31252 | — | — | 1 | 7.26 |
| CHEMBL289898 | — | — | 1 | 7.06 |
| CHEMBL31886 | — | — | 1 | 7.04 |
| CHEMBL418034 | — | — | 1 | 7.00 |
| CHEMBL31587 | — | — | 1 | 6.80 |
| CHEMBL418031 | — | — | 1 | 6.80 |
| CHEMBL286580 | — | — | 1 | 6.68 |
| CHEMBL30755 | — | — | 1 | 6.66 |
| CHEMBL287637 | — | — | 1 | 6.66 |
| CHEMBL287139 | — | — | 1 | 6.27 |
| CHEMBL283237 | — | — | 1 | 6.24 |
| CHEMBL440654 | — | — | 1 | 6.13 |
| CHEMBL442264 | — | — | 1 | 6.06 |
| CHEMBL431689 | — | — | 1 | 5.58 |
| CHEMBL31479 | — | — | 1 | 4.58 |
| CHEMBL286733 | — | — | 1 | 4.40 |
| CHEMBL413256 | — | — | 1 | 4.30 |
| CHEMBL31997 | — | — | 1 | - |
| CHEMBL417673 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31601 | REMIKIREN | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL430539 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL417485 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL31466 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL285454 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL431502 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL283683 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL31252 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL289898 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL31886 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL418034 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL31587 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL418031 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL286580 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL30755 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL287637 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL287139 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL283237 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL440654 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL442264 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL431689 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL31479 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL286733 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL413256 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL31997 | — | IC50 | = | 1200000.0 | nM | - |
| CHEMBL417673 | — | IC50 | > | 1000000.0 | nM | - |