Assay Detail
Binding
CHEMBL828351
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against porcine prolyl oligopeptidase by using 4 mM Suc-Gly-Pro-7-amido-4-methylcoumarin as substrate (pH 7.0) at 30 degree C for 60 min
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 8.01 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76578 | — | — | 1 | 9.70 |
| CHEMBL189620 | — | — | 1 | 9.66 |
| CHEMBL362971 | — | — | 1 | 9.66 |
| CHEMBL435223 | — | — | 1 | 9.49 |
| CHEMBL79993 | Z-PRO-PROLINAL | — | 1 | 9.48 |
| CHEMBL141588 | — | — | 1 | 9.41 |
| CHEMBL370320 | — | — | 1 | 9.41 |
| CHEMBL343570 | — | — | 1 | 9.24 |
| CHEMBL187844 | — | — | 1 | 9.21 |
| CHEMBL364335 | — | — | 1 | 9.14 |
| CHEMBL189807 | — | — | 1 | 9.12 |
| CHEMBL191572 | — | — | 1 | 8.96 |
| CHEMBL188862 | — | — | 1 | 8.92 |
| CHEMBL188710 | — | — | 1 | 8.92 |
| CHEMBL364989 | — | — | 1 | 8.89 |
| CHEMBL335815 | — | — | 1 | 8.89 |
| CHEMBL140461 | — | — | 1 | 8.82 |
| CHEMBL425001 | — | — | 1 | 8.80 |
| CHEMBL188379 | — | — | 1 | 8.80 |
| CHEMBL289651 | — | — | 1 | 8.66 |
| CHEMBL363383 | — | — | 1 | 8.54 |
| CHEMBL363655 | — | — | 1 | 8.51 |
| CHEMBL187830 | — | — | 1 | 8.38 |
| CHEMBL188501 | — | — | 1 | 8.34 |
| CHEMBL191061 | — | — | 1 | 8.16 |
| CHEMBL140623 | — | — | 1 | 7.89 |
| CHEMBL362492 | — | — | 1 | 7.85 |
| CHEMBL187723 | — | — | 1 | 7.75 |
| CHEMBL188259 | — | — | 1 | 7.64 |
| CHEMBL141158 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76578 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL189620 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL362971 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL435223 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL79993 | Z-PRO-PROLINAL | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL141588 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL370320 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL343570 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL187844 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL364335 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL189807 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL191572 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL188862 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL188710 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL335815 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL364989 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL140461 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL425001 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL188379 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL289651 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL363383 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL363655 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL187830 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL188501 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL191061 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL140623 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL362492 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL187723 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL188259 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL141158 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL188468 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL311364 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL187502 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL534924 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL140310 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL190271 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL191338 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL365969 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL343739 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL189765 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL191187 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL370722 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL362737 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL187934 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL188317 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL371853 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL188390 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL362534 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL139617 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL364930 | — | IC50 | = | 1200.0 | nM | 5.92 |