Assay Detail
Binding
CHEMBL4339144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured after 1 hr by fluorescence based assay
31
Total Activities
31
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
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.44 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3703484 | — | — | 1 | 9.52 |
| CHEMBL3676144 | — | — | 1 | 9.42 |
| CHEMBL4443138 | — | — | 1 | 9.10 |
| CHEMBL3676150 | — | — | 1 | 8.82 |
| CHEMBL4557208 | — | — | 1 | 8.80 |
| CHEMBL4442804 | — | — | 1 | 8.70 |
| CHEMBL3676141 | — | — | 1 | 8.35 |
| CHEMBL4518426 | — | — | 1 | 8.27 |
| CHEMBL417007 | LBQ-657 | -1.0 | 1 | 8.22 |
| CHEMBL3676140 | — | — | 1 | 8.17 |
| CHEMBL4466321 | — | — | 1 | 8.16 |
| CHEMBL4474653 | — | — | 1 | 8.10 |
| CHEMBL4439270 | — | — | 1 | 7.70 |
| CHEMBL4592467 | — | — | 1 | 7.67 |
| CHEMBL4434901 | — | — | 1 | 7.62 |
| CHEMBL3676155 | — | — | 1 | 7.60 |
| CHEMBL4568947 | — | — | 1 | 7.58 |
| CHEMBL4475874 | — | — | 1 | 7.36 |
| CHEMBL4459630 | — | — | 1 | 7.27 |
| CHEMBL4518025 | — | — | 1 | 7.22 |
| CHEMBL4547205 | — | — | 1 | 6.96 |
| CHEMBL4443565 | — | — | 1 | 6.67 |
| CHEMBL4448802 | — | — | 1 | 6.56 |
| CHEMBL4564942 | — | — | 1 | 6.38 |
| CHEMBL46081 | — | — | 1 | 6.26 |
| CHEMBL4471166 | — | — | 1 | 6.10 |
| CHEMBL4559586 | — | — | 1 | 5.86 |
| CHEMBL4465277 | — | — | 1 | 5.82 |
| CHEMBL4458213 | — | — | 1 | 5.71 |
| CHEMBL4548017 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3703484 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3676144 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4443138 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3676150 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4557208 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4442804 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3676141 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4518426 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL417007 | LBQ-657 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3676140 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4466321 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4474653 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4439270 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4592467 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL4434901 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3676155 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4568947 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4475874 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4459630 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4518025 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4547205 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL4443565 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4448802 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4564942 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL46081 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4471166 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL4559586 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4465277 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4458213 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4548017 | — | IC50 | = | 4182.0 | nM | 5.38 |
| CHEMBL4550194 | — | IC50 | = | 4862.0 | nM | 5.31 |