Assay Detail
Binding
CHEMBL616877
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human cloned 5-hydroxytryptamine receptor 2A in HEK293 cells, using [3H]ketanserin 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 | 6.40 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14345 | — | — | 1 | 7.20 |
| CHEMBL14863 | — | — | 1 | 7.20 |
| CHEMBL428879 | — | — | 1 | 7.10 |
| CHEMBL14726 | — | — | 1 | 7.00 |
| CHEMBL14864 | — | — | 1 | 7.00 |
| CHEMBL14276 | — | — | 1 | 6.90 |
| CHEMBL14841 | — | — | 1 | 6.80 |
| CHEMBL14460 | SB-243213 | — | 1 | 6.80 |
| CHEMBL14563 | SB-242084 | — | 1 | 6.80 |
| CHEMBL14255 | — | — | 1 | 6.70 |
| CHEMBL276571 | — | — | 1 | 6.70 |
| CHEMBL274066 | — | — | 1 | 6.70 |
| CHEMBL416896 | — | — | 1 | 6.70 |
| CHEMBL273345 | — | — | 1 | 6.60 |
| CHEMBL14401 | — | — | 1 | 6.60 |
| CHEMBL14458 | — | — | 1 | 6.60 |
| CHEMBL417082 | — | — | 1 | 6.60 |
| CHEMBL14462 | — | — | 1 | 6.40 |
| CHEMBL14548 | — | — | 1 | 6.30 |
| CHEMBL14076 | — | — | 1 | 6.30 |
| CHEMBL280297 | — | — | 1 | 6.20 |
| CHEMBL14374 | — | — | 1 | 6.10 |
| CHEMBL14352 | — | — | 1 | 6.00 |
| CHEMBL446942 | — | — | 1 | 6.00 |
| CHEMBL277732 | — | — | 1 | 5.90 |
| CHEMBL14469 | — | — | 1 | 5.90 |
| CHEMBL280465 | — | — | 1 | 5.80 |
| CHEMBL14652 | — | — | 1 | 5.80 |
| CHEMBL278267 | — | — | 1 | 5.40 |
| CHEMBL14606 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14345 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL14863 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL428879 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL14726 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL14864 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL14276 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL14841 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL14460 | SB-243213 | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL14563 | SB-242084 | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL276571 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL416896 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL274066 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL14255 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL417082 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL14458 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL273345 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL14401 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL14462 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL14548 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL14076 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL280297 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL14374 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL14352 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL446942 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL277732 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL14469 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL280465 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL14652 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL278267 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL14606 | — | Ki | = | 5011.87 | nM | 5.30 |
| CHEMBL280322 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL14362 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL278685 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL14111 | — | Ki | < | 6309.57 | nM | - |
| CHEMBL274692 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL14368 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL277111 | — | Ki | < | 10000.0 | nM | - |