Assay Detail
Binding
CHEMBL4056822
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Inhibition of recombinant human neprilysin using Suc-Ala-Ala-Phe-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence assay
37
Total Activities
37
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
Substituted α-mercaptoketones, new types of specific neprilysin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.33 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075182 | — | — | 1 | 8.70 |
| CHEMBL4091227 | — | — | 1 | 8.38 |
| CHEMBL4080935 | — | — | 1 | 8.34 |
| CHEMBL4089776 | — | — | 1 | 8.15 |
| CHEMBL4069278 | — | — | 1 | 8.05 |
| CHEMBL4077560 | — | — | 1 | 7.92 |
| CHEMBL4085997 | — | — | 1 | 7.75 |
| CHEMBL4066184 | — | — | 1 | 7.70 |
| CHEMBL4075187 | — | — | 1 | 7.66 |
| CHEMBL19621 | — | — | 1 | 7.64 |
| CHEMBL4073385 | — | — | 1 | 7.58 |
| CHEMBL4066384 | — | — | 1 | 7.54 |
| CHEMBL4074531 | — | — | 1 | 7.52 |
| CHEMBL4096514 | — | — | 1 | 7.50 |
| CHEMBL4070297 | — | — | 1 | 7.44 |
| CHEMBL4094037 | — | — | 1 | 7.44 |
| CHEMBL4074608 | — | — | 1 | 7.40 |
| CHEMBL4087357 | — | — | 1 | 7.34 |
| CHEMBL4067507 | — | — | 1 | 7.31 |
| CHEMBL4086067 | — | — | 1 | 7.30 |
| CHEMBL4088816 | — | — | 1 | 7.28 |
| CHEMBL4102672 | — | — | 1 | 7.27 |
| CHEMBL4078411 | — | — | 1 | 7.27 |
| CHEMBL4098968 | — | — | 1 | 7.21 |
| CHEMBL4095593 | — | — | 1 | 7.21 |
| CHEMBL4064153 | — | — | 1 | 7.11 |
| CHEMBL4088709 | — | — | 1 | 7.07 |
| CHEMBL4075680 | — | — | 1 | 7.02 |
| CHEMBL4094929 | — | — | 1 | 7.02 |
| CHEMBL4100250 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075182 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4091227 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL4080935 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL4089776 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4069278 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4077560 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4085997 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4066184 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4075187 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL19621 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4073385 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4066384 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4074531 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4096514 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4094037 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4070297 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4074608 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4087357 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4067507 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4086067 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4088816 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4102672 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4078411 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4098968 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4095593 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4064153 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4088709 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL4094929 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL4075680 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL4100250 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4061434 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL4082357 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL4101421 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4067370 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL4091335 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL4063351 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL4076819 | — | Ki | > | 1e-05 | nM | - |