Assay Detail
Binding
CHEMBL5578802
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Inhibition of OGA in rat PC12 cells assessed as OGlcNAcylated protein level incubated for 24 hrs by ELISA
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | PC12 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-(Arylethynyl)piperidine Derivatives as Potent Nonsaccharide <i>O</i>-GlcNAcase Inhibitors for the Treatment of Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 7.32 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5584048 | — | — | 1 | 8.16 |
| CHEMBL5591513 | — | — | 1 | 8.13 |
| CHEMBL5592023 | — | — | 1 | 7.97 |
| CHEMBL5593511 | — | — | 1 | 7.88 |
| CHEMBL5594139 | — | — | 1 | 7.68 |
| CHEMBL5592978 | — | — | 1 | 7.65 |
| CHEMBL5591099 | — | — | 1 | 7.61 |
| CHEMBL5591879 | — | — | 1 | 7.58 |
| CHEMBL5591488 | — | — | 1 | 7.55 |
| CHEMBL5592529 | — | — | 1 | 7.50 |
| CHEMBL5592778 | — | — | 1 | 7.48 |
| CHEMBL5590598 | — | — | 1 | 7.31 |
| CHEMBL5593700 | — | — | 1 | 7.29 |
| CHEMBL5594475 | — | — | 1 | 7.26 |
| CHEMBL5593786 | — | — | 1 | 7.22 |
| CHEMBL5591200 | — | — | 1 | 7.21 |
| CHEMBL5591704 | — | — | 1 | 7.07 |
| CHEMBL5590996 | — | — | 1 | 7.04 |
| CHEMBL5591460 | — | — | 1 | 7.04 |
| CHEMBL5583946 | — | — | 1 | 7.01 |
| CHEMBL5595991 | — | — | 1 | 7.01 |
| CHEMBL5591551 | — | — | 1 | 6.97 |
| CHEMBL5590780 | — | — | 1 | 6.73 |
| CHEMBL5594381 | — | — | 1 | 6.69 |
| CHEMBL5590193 | — | — | 1 | 6.00 |
| CHEMBL5592188 | — | — | 1 | - |
| CHEMBL5592881 | — | — | 1 | - |
| CHEMBL5591707 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5584048 | — | EC50 | = | 6.85 | nM | 8.16 |
| CHEMBL5591513 | — | EC50 | = | 7.47 | nM | 8.13 |
| CHEMBL5592023 | — | EC50 | = | 10.61 | nM | 7.97 |
| CHEMBL5593511 | — | EC50 | = | 13.24 | nM | 7.88 |
| CHEMBL5594139 | — | EC50 | = | 20.69 | nM | 7.68 |
| CHEMBL5592978 | — | EC50 | = | 22.62 | nM | 7.65 |
| CHEMBL5591099 | — | EC50 | = | 24.59 | nM | 7.61 |
| CHEMBL5591879 | — | EC50 | = | 26.2 | nM | 7.58 |
| CHEMBL5591488 | — | EC50 | = | 27.93 | nM | 7.55 |
| CHEMBL5592529 | — | EC50 | = | 31.84 | nM | 7.50 |
| CHEMBL5592778 | — | EC50 | = | 33.01 | nM | 7.48 |
| CHEMBL5590598 | — | EC50 | = | 48.51 | nM | 7.31 |
| CHEMBL5593700 | — | EC50 | = | 51.56 | nM | 7.29 |
| CHEMBL5594475 | — | EC50 | = | 54.45 | nM | 7.26 |
| CHEMBL5593786 | — | EC50 | = | 60.67 | nM | 7.22 |
| CHEMBL5591200 | — | EC50 | = | 62.34 | nM | 7.21 |
| CHEMBL5591704 | — | EC50 | = | 85.52 | nM | 7.07 |
| CHEMBL5590996 | — | EC50 | = | 90.44 | nM | 7.04 |
| CHEMBL5591460 | — | EC50 | = | 90.72 | nM | 7.04 |
| CHEMBL5583946 | — | EC50 | = | 96.86 | nM | 7.01 |
| CHEMBL5595991 | — | EC50 | = | 98.12 | nM | 7.01 |
| CHEMBL5591551 | — | EC50 | = | 106.3 | nM | 6.97 |
| CHEMBL5590780 | — | EC50 | = | 184.3 | nM | 6.73 |
| CHEMBL5594381 | — | EC50 | = | 205.2 | nM | 6.69 |
| CHEMBL5590193 | — | EC50 | = | 993.1 | nM | 6.00 |
| CHEMBL5592188 | — | EC50 | - | — | - | |
| CHEMBL5592881 | — | EC50 | - | — | - | |
| CHEMBL5591707 | — | EC50 | - | — | - |