Assay Detail
Binding
CHEMBL617754
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Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| Ki | 37 | 8.56 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14111 | — | — | 1 | 9.50 |
| CHEMBL14864 | — | — | 1 | 9.40 |
| CHEMBL417082 | — | — | 1 | 9.30 |
| CHEMBL276571 | — | — | 1 | 9.30 |
| CHEMBL14374 | — | — | 1 | 9.20 |
| CHEMBL14362 | — | — | 1 | 9.20 |
| CHEMBL273345 | — | — | 1 | 9.20 |
| CHEMBL416896 | — | — | 1 | 9.20 |
| CHEMBL280465 | — | — | 1 | 9.20 |
| CHEMBL14863 | — | — | 1 | 9.20 |
| CHEMBL14345 | — | — | 1 | 9.10 |
| CHEMBL14563 | SB-242084 | — | 1 | 9.00 |
| CHEMBL14460 | SB-243213 | — | 1 | 9.00 |
| CHEMBL14276 | — | — | 1 | 9.00 |
| CHEMBL14255 | — | — | 1 | 9.00 |
| CHEMBL14606 | — | — | 1 | 9.00 |
| CHEMBL14726 | — | — | 1 | 8.90 |
| CHEMBL428879 | — | — | 1 | 8.80 |
| CHEMBL14368 | — | — | 1 | 8.70 |
| CHEMBL274066 | — | — | 1 | 8.60 |
| CHEMBL280297 | — | — | 1 | 8.60 |
| CHEMBL446942 | — | — | 1 | 8.50 |
| CHEMBL14841 | — | — | 1 | 8.50 |
| CHEMBL14469 | — | — | 1 | 8.30 |
| CHEMBL14076 | — | — | 1 | 8.30 |
| CHEMBL277111 | — | — | 1 | 8.30 |
| CHEMBL274692 | — | — | 1 | 8.30 |
| CHEMBL14652 | — | — | 1 | 8.30 |
| CHEMBL14401 | — | — | 1 | 8.20 |
| CHEMBL14458 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14111 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL14864 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL276571 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL417082 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL14374 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL14362 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL273345 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL416896 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL280465 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL14863 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL14345 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL14255 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL14276 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL14606 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL14460 | SB-243213 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL14563 | SB-242084 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL14726 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL428879 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL14368 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL280297 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL274066 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL446942 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL14841 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL14469 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL14076 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL277111 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL274692 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL14652 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL14401 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL14458 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL14352 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL278267 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL14548 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL278685 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL14462 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL277732 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL280322 | — | Ki | = | 1995.26 | nM | 5.70 |