Assay Detail
Functional
CHEMBL617620
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Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 6.21 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.90 |
| CHEMBL143027 | — | — | 1 | 6.61 |
| CHEMBL142668 | — | — | 1 | 6.36 |
| CHEMBL142316 | — | — | 1 | 6.23 |
| CHEMBL358895 | — | — | 1 | 6.19 |
| CHEMBL357517 | — | — | 1 | 5.74 |
| CHEMBL143937 | — | — | 1 | 5.46 |
| CHEMBL141600 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL143027 | — | Kd | = | 245.47 | nM | 6.61 |
| CHEMBL142668 | — | Kd | = | 436.52 | nM | 6.36 |
| CHEMBL142316 | — | Kd | = | 588.84 | nM | 6.23 |
| CHEMBL358895 | — | Kd | = | 645.65 | nM | 6.19 |
| CHEMBL357517 | — | Kd | = | 1819.7 | nM | 5.74 |
| CHEMBL143937 | — | Kd | = | 3467.37 | nM | 5.46 |
| CHEMBL141600 | — | Kd | > | 100000.0 | nM | - |