Assay Detail
Binding
CHEMBL765791
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In vitro inhibitory activity against purified prolyl endopeptidase (PEP) from canine brain.
37
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.61 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302654 | — | — | 1 | 9.38 |
| CHEMBL65284 | — | — | 1 | 9.35 |
| CHEMBL291393 | — | — | 1 | 9.34 |
| CHEMBL63745 | — | — | 1 | 9.28 |
| CHEMBL294367 | — | — | 1 | 9.26 |
| CHEMBL65512 | — | — | 1 | 9.07 |
| CHEMBL65338 | — | — | 1 | 9.00 |
| CHEMBL79993 | Z-PRO-PROLINAL | — | 1 | 8.96 |
| CHEMBL66088 | — | — | 1 | 8.96 |
| CHEMBL62580 | — | — | 1 | 8.92 |
| CHEMBL304644 | — | — | 1 | 8.64 |
| CHEMBL65109 | — | — | 1 | 8.47 |
| CHEMBL66257 | — | — | 1 | 8.40 |
| CHEMBL63045 | — | — | 1 | 8.27 |
| CHEMBL66258 | — | — | 1 | 8.19 |
| CHEMBL64240 | — | — | 1 | 8.06 |
| CHEMBL62960 | — | — | 1 | 8.00 |
| CHEMBL262241 | — | — | 1 | 7.77 |
| CHEMBL304020 | — | — | 1 | 7.75 |
| CHEMBL63133 | — | — | 1 | 7.62 |
| CHEMBL303066 | — | — | 1 | 7.44 |
| CHEMBL63994 | — | — | 1 | 7.42 |
| CHEMBL63537 | — | — | 1 | 7.40 |
| CHEMBL292302 | — | — | 1 | 7.32 |
| CHEMBL289651 | — | — | 1 | 7.31 |
| CHEMBL416866 | — | — | 1 | 7.22 |
| CHEMBL65373 | — | — | 1 | 7.16 |
| CHEMBL23089 | — | — | 1 | 7.07 |
| CHEMBL293168 | — | — | 1 | 6.89 |
| CHEMBL413107 | — | — | 2 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302654 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL65284 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL291393 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL63745 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL294367 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL65512 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL65338 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL79993 | Z-PRO-PROLINAL | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL66088 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL62580 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL304644 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL65109 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL66257 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL63045 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL66258 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL64240 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL62960 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL262241 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL304020 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL63133 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL303066 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL63994 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL63537 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL292302 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL289651 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL416866 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL65373 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL23089 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL293168 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL413107 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL413107 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL304892 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL62629 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL294803 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL65463 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL65561 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL302398 | — | IC50 | = | 94000.0 | nM | 4.03 |