Assay Detail
Binding
CHEMBL617224
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Binding affinity against serotonin 5-hydroxytryptamine 2 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.34 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304902 | CLOTHIAPINE | 2.0 | 1 | 9.23 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 8.75 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.48 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.41 |
| CHEMBL63756 | FLUPERLAPINE | 2.0 | 1 | 8.41 |
| CHEMBL67284 | ISOCLOTHIAPINE | — | 1 | 8.38 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.63 |
| CHEMBL149240 | — | — | 1 | 7.35 |
| CHEMBL433744 | — | — | 1 | 7.35 |
| CHEMBL147463 | — | — | 1 | 7.19 |
| CHEMBL151809 | — | — | 1 | 7.01 |
| CHEMBL151263 | — | — | 1 | 6.55 |
| CHEMBL356076 | — | — | 1 | 6.29 |
| CHEMBL435441 | — | — | 1 | 5.94 |
| CHEMBL146741 | — | — | 1 | 5.85 |
| CHEMBL149108 | — | — | 1 | 4.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304902 | CLOTHIAPINE | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL415300 | ISOCLOZAPINE | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL42 | CLOZAPINE | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL63756 | FLUPERLAPINE | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL67284 | ISOCLOTHIAPINE | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL149240 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL433744 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL147463 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL151809 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL151263 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL356076 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL435441 | — | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL146741 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL149108 | — | Ki | = | 22387.21 | nM | 4.65 |