Assay Detail
Binding
CHEMBL5578422
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Inhibition of human NEU1 expressed in HEK293 cells using 4-MUNANA as substrate preincubated with compound for 0.25 hrs followed by substrate addition and measured after 0.5 hrs by fluorescence based analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bioisosteres at C9 of 2-Deoxy-2,3-didehydro-<i>N</i>-acetyl Neuraminic Acid Identify Selective Inhibitors of NEU3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.68 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4294428 | — | — | 1 | 5.30 |
| CHEMBL5594004 | — | — | 1 | 4.92 |
| CHEMBL96712 | NEU5AC2EN | — | 1 | 4.68 |
| CHEMBL5594290 | — | — | 1 | 4.60 |
| CHEMBL5591566 | — | — | 1 | 4.46 |
| CHEMBL5583781 | — | — | 1 | 4.40 |
| CHEMBL4285561 | — | — | 1 | 4.40 |
| CHEMBL5590354 | — | — | 1 | - |
| CHEMBL5590360 | — | — | 1 | - |
| CHEMBL4076203 | — | — | 1 | - |
| CHEMBL5590001 | — | — | 1 | - |
| CHEMBL5591326 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4294428 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5594004 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL96712 | NEU5AC2EN | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL5594290 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5591566 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL5583781 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4285561 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL5590354 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL5590360 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL4076203 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5590001 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5591326 | — | IC50 | > | 500000.0 | nM | - |