Assay Detail
ADMET
CHEMBL663530
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Inhibition of heterologously expressed human cytochrome P450 2D6
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.82 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276140 | — | — | 1 | 6.96 |
| CHEMBL14276 | — | — | 1 | 4.68 |
| CHEMBL14563 | SB-242084 | — | 1 | - |
| CHEMBL14460 | SB-243213 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276140 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL14276 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL14563 | SB-242084 | IC50 | > | 100000.0 | nM | - |
| CHEMBL14460 | SB-243213 | IC50 | > | 100000.0 | nM | - |