Assay Detail
Binding
CHEMBL4411114
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Inhibition of PREP in C57BL/6 mouse cortex homogenate assessed as formation of 7-amido-4-methylcoumarin using Suc-Gly-Pro-amido-4-methylcoumarin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorometric assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.13 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189620 | — | — | 1 | 9.52 |
| CHEMBL4549821 | — | — | 1 | 8.48 |
| CHEMBL4528594 | — | — | 1 | 7.04 |
| CHEMBL4465322 | — | — | 1 | 6.58 |
| CHEMBL4556841 | — | — | 1 | 6.53 |
| CHEMBL4540171 | — | — | 1 | 5.29 |
| CHEMBL4588059 | — | — | 1 | 5.21 |
| CHEMBL4586782 | — | — | 1 | 4.92 |
| CHEMBL4520738 | — | — | 1 | 4.87 |
| CHEMBL4475037 | — | — | 1 | 4.54 |
| CHEMBL4551013 | — | — | 1 | 4.45 |
| CHEMBL4441906 | — | — | 1 | - |
| CHEMBL4436952 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189620 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4549821 | — | IC50 | = | 3.28 | nM | 8.48 |
| CHEMBL4528594 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4465322 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4556841 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL4540171 | — | IC50 | = | 5141.0 | nM | 5.29 |
| CHEMBL4588059 | — | IC50 | = | 6213.0 | nM | 5.21 |
| CHEMBL4586782 | — | IC50 | = | 12080.0 | nM | 4.92 |
| CHEMBL4520738 | — | IC50 | = | 13510.0 | nM | 4.87 |
| CHEMBL4475037 | — | IC50 | = | 28800.0 | nM | 4.54 |
| CHEMBL4551013 | — | IC50 | = | 35180.0 | nM | 4.45 |
| CHEMBL4441906 | — | IC50 | = | 153800.0 | nM | - |
| CHEMBL4436952 | — | IC50 | = | 457000.0 | nM | - |