Assay Detail
Binding
CHEMBL3223375
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NEP using N-Dansyl-D-Ala-Gly-p-nitro-Phe-Gly as substrate preincubated for 10 mins followed by substrate addition measured after 2 hrs by spectrophotometric analysis
14
Total Activities
14
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
Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.91 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.89 |
| CHEMBL3221965 | — | — | 1 | 7.20 |
| CHEMBL3221963 | — | — | 1 | 6.10 |
| CHEMBL3221958 | — | — | 1 | 5.60 |
| CHEMBL3222111 | — | — | 1 | 5.20 |
| CHEMBL3221959 | — | — | 1 | 4.30 |
| CHEMBL3221954 | — | — | 1 | 4.10 |
| CHEMBL3221955 | — | — | 1 | - |
| CHEMBL3221956 | — | — | 1 | - |
| CHEMBL3221957 | — | — | 1 | - |
| CHEMBL3221960 | — | — | 1 | - |
| CHEMBL3221961 | — | — | 1 | - |
| CHEMBL3221962 | — | — | 1 | - |
| CHEMBL3221964 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10247 | THIORPHAN | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3221965 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3221963 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3221958 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3222111 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3221959 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3221954 | — | IC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL3221955 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221956 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221957 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221960 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221961 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221962 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3221964 | — | IC50 | > | 1000000.0 | nM | - |