Assay Detail
Binding
CHEMBL3707552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Previously, one of the following compounds discussed below have been studied in memapsin 2 inhibition (Ghosh et al., 2008), which the others are previously unpublished. Given the closely related substrate specificity for memapsin 1 and memapsin 2, the inventors chose to screen these previously identified memapsin 2 inhibitors for lead compounds as memapsin 1 inhibitors. Recombinant memapsin 1 ectodomain was prepared as described by Turner et al. (2002) and assayed using a commercially purchased fluorescent substrate.
6
Total Activities
6
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
Inhibition of memapsin 1 cleavage in the treatment of diabetes
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.22 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3664021 | — | — | 1 | 8.18 |
| CHEMBL3664020 | — | — | 1 | 6.57 |
| CHEMBL3704768 | — | — | 1 | 6.25 |
| CHEMBL3704770 | — | — | 1 | 5.78 |
| CHEMBL3664019 | — | — | 1 | 5.28 |
| CHEMBL3664018 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3664021 | — | Ki | = | 6.56 | nM | 8.18 |
| CHEMBL3664020 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL3704768 | — | Ki | = | 563.5 | nM | 6.25 |
| CHEMBL3704770 | — | Ki | = | 1657.0 | nM | 5.78 |
| CHEMBL3664019 | — | Ki | = | 5245.0 | nM | 5.28 |
| CHEMBL3664018 | — | Ki | = | 5812.0 | nM | 5.24 |