Assay Detail
Binding
CHEMBL4329997
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Inhibition of recombinant human His6-tagged HexB expressed in Pichia pastoris using varying levels of 4-Mu-GlcNAc as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by dixon plot analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Modification of the Thioglycosyl-Naphthalimides as Potent and Selective Human O-GlcNAcase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.34 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448965 | — | — | 1 | 5.92 |
| CHEMBL4452208 | — | — | 1 | 5.80 |
| CHEMBL4435797 | — | — | 1 | 5.80 |
| CHEMBL4454357 | — | — | 1 | 5.75 |
| CHEMBL4548064 | — | — | 1 | 5.75 |
| CHEMBL4548738 | — | — | 1 | 5.58 |
| CHEMBL4555514 | — | — | 1 | 5.36 |
| CHEMBL4540913 | — | — | 1 | 5.29 |
| CHEMBL4438655 | — | — | 1 | 4.66 |
| CHEMBL4474777 | — | — | 1 | 4.61 |
| CHEMBL4559735 | — | — | 1 | 4.25 |
| CHEMBL4564023 | — | — | 1 | - |
| CHEMBL4440132 | — | — | 1 | - |
| CHEMBL4455894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448965 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL4452208 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4435797 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4454357 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4548064 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4548738 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL4555514 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL4540913 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL4438655 | — | Ki | = | 22100.0 | nM | 4.66 |
| CHEMBL4474777 | — | Ki | = | 24700.0 | nM | 4.61 |
| CHEMBL4559735 | — | Ki | = | 56200.0 | nM | 4.25 |
| CHEMBL4564023 | — | Ki | - | — | - | |
| CHEMBL4440132 | — | Ki | - | — | - | |
| CHEMBL4455894 | — | Ki | - | — | - |