Assay Detail
ADMET
CHEMBL666157
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Inhibition of heterologously expressed human cytochrome P450 1A2.
22
Total Activities
22
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 | 22 | 5.30 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14352 | — | — | 1 | 7.70 |
| CHEMBL14864 | — | — | 1 | 6.70 |
| CHEMBL417082 | — | — | 1 | 5.70 |
| CHEMBL14652 | — | — | 1 | 5.58 |
| CHEMBL276571 | — | — | 1 | 5.52 |
| CHEMBL14548 | — | — | 1 | 5.52 |
| CHEMBL14726 | — | — | 1 | 5.40 |
| CHEMBL14255 | — | — | 1 | 5.40 |
| CHEMBL416896 | — | — | 1 | 5.22 |
| CHEMBL14606 | — | — | 1 | 5.16 |
| CHEMBL277111 | — | — | 1 | 5.16 |
| CHEMBL14368 | — | — | 1 | 5.16 |
| CHEMBL273345 | — | — | 1 | 5.10 |
| CHEMBL14362 | — | — | 1 | 4.96 |
| CHEMBL14276 | — | — | 1 | 4.55 |
| CHEMBL14863 | — | — | 1 | 4.30 |
| CHEMBL14469 | — | — | 1 | 4.14 |
| CHEMBL14345 | — | — | 1 | 4.11 |
| CHEMBL278267 | — | — | 1 | - |
| CHEMBL14111 | — | — | 1 | - |
| CHEMBL280297 | — | — | 1 | - |
| CHEMBL14374 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14352 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL14864 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL417082 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL14652 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL276571 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL14548 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL14726 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL14255 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL416896 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL14606 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL277111 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL14368 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL273345 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL14362 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL14276 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL14863 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL14469 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL14345 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL278267 | — | IC50 | = | - | nM | - |
| CHEMBL14111 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL280297 | — | IC50 | = | - | nM | - |
| CHEMBL14374 | — | IC50 | > | 100000.0 | nM | - |