Assay Detail
Binding
CHEMBL661107
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Inhibition of Catechol O-methyltransferase activity in rat brain
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.33 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1324 | TOLCAPONE | 4.0 | 1 | 8.66 |
| CHEMBL160038 | NEBICAPONE | 2.0 | 1 | 8.43 |
| CHEMBL953 | ENTACAPONE | 4.0 | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1324 | TOLCAPONE | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL160038 | NEBICAPONE | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL953 | ENTACAPONE | IC50 | = | 12.8 | nM | 7.89 |