Assay Detail
Binding
CHEMBL4411113
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Inhibition of recombinant porcine brain PREP expressed in Escherichia coli 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
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| 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 | 15 | 6.69 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189620 | — | — | 1 | 9.07 |
| CHEMBL4549821 | — | — | 1 | 8.39 |
| CHEMBL4470147 | — | — | 1 | 8.27 |
| CHEMBL289651 | — | — | 1 | 7.92 |
| CHEMBL4446414 | — | — | 1 | 7.92 |
| CHEMBL4528594 | — | — | 1 | 6.89 |
| CHEMBL4529226 | — | — | 1 | 6.83 |
| CHEMBL4465322 | — | — | 1 | 6.66 |
| CHEMBL4536787 | — | — | 1 | 6.57 |
| CHEMBL4552659 | — | — | 1 | 5.44 |
| CHEMBL4520974 | — | — | 1 | 5.36 |
| CHEMBL4521222 | — | — | 1 | 4.97 |
| CHEMBL4483620 | — | — | 1 | 4.76 |
| CHEMBL4464018 | — | — | 1 | 4.57 |
| CHEMBL4520852 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189620 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL4549821 | — | IC50 | = | 4.06 | nM | 8.39 |
| CHEMBL4470147 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL289651 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4446414 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4528594 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4529226 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL4465322 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4536787 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4552659 | — | IC50 | = | 3626.0 | nM | 5.44 |
| CHEMBL4520974 | — | IC50 | = | 4371.0 | nM | 5.36 |
| CHEMBL4521222 | — | IC50 | = | 10640.0 | nM | 4.97 |
| CHEMBL4483620 | — | IC50 | = | 17540.0 | nM | 4.76 |
| CHEMBL4464018 | — | IC50 | = | 27180.0 | nM | 4.57 |
| CHEMBL4520852 | — | IC50 | = | 205400.0 | nM | - |