Assay Detail
Binding
CHEMBL1120467
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Displacement of [3H]mesulergine from human 5HT2C receptor expressed CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.26 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1084721 | — | — | 1 | 8.15 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 7.89 |
| CHEMBL1086507 | — | — | 1 | 7.68 |
| CHEMBL358075 | — | — | 1 | 7.41 |
| CHEMBL1082467 | — | — | 1 | 7.39 |
| CHEMBL1084976 | — | — | 1 | 7.33 |
| CHEMBL1082773 | — | — | 1 | 7.19 |
| CHEMBL175832 | — | — | 1 | 7.16 |
| CHEMBL210230 | — | — | 1 | 7.00 |
| CHEMBL1083416 | — | — | 1 | 6.90 |
| CHEMBL1082452 | — | — | 1 | 6.74 |
| CHEMBL1083415 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1084721 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1086507 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL358075 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1082467 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1084976 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL1082773 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL175832 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL210230 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1083416 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL1082452 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL1083415 | — | Ki | = | 526.0 | nM | 6.28 |