Assay Detail
Binding
CHEMBL3706013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubated with test compounds at various concentrations for 1 hour at room temperature in 10 mM sodium phosphate buffer at pH 7.4, containing 150 mM NaCl and 0.05% (w/v) CHAPS. The enzymatic reaction is started by the addition of a synthetic peptide substrate Cys(PT14)-Arg-Arg-Leu-Trp-OH to a final concentration of 0.7 μM. Substrate hydrolysis leads to an increase fluorescence lifetime (FLT) of PT14 measured by the means of a FLT reader as described by Doering et al. (2009). The effect of the compound on the enzymatic activity was determined after 1 hour (t=60 min) incubation at room temperature.
22
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Membrane metallo-endopeptidase-like 1 (CHEMBL3638356) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted aminopropionic derivatives as neprilysin inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.44 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3676152 | — | — | 1 | 10.15 |
| CHEMBL3676150 | — | — | 2 | 9.70 |
| CHEMBL3676151 | — | — | 1 | 9.30 |
| CHEMBL3676145 | — | — | 1 | 9.30 |
| CHEMBL3676147 | — | — | 1 | 9.15 |
| CHEMBL3676144 | — | — | 1 | 9.15 |
| CHEMBL3676153 | — | — | 1 | 9.10 |
| CHEMBL3676154 | — | — | 1 | 8.92 |
| CHEMBL3676143 | — | — | 1 | 8.64 |
| CHEMBL3676146 | — | — | 1 | 8.57 |
| CHEMBL3639750 | — | — | 1 | 8.52 |
| CHEMBL3676141 | — | — | 1 | 8.40 |
| CHEMBL3676140 | — | — | 1 | 8.15 |
| CHEMBL3676139 | — | — | 1 | 7.82 |
| CHEMBL3676138 | — | — | 1 | 7.82 |
| CHEMBL3676137 | — | — | 1 | 7.75 |
| CHEMBL3676155 | — | — | 2 | 7.42 |
| CHEMBL3676149 | — | — | 1 | 7.25 |
| CHEMBL3676142 | — | — | 1 | 7.17 |
| CHEMBL3676148 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3676152 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3676150 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3676151 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3676145 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3676147 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3676144 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3676153 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3676150 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3676154 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3676143 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3676146 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3639750 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3676141 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3676140 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3676139 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3676138 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3676137 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3676155 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3676155 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3676149 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3676142 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3676148 | — | IC50 | = | 75.0 | nM | 7.12 |