Assay Detail
Binding
CHEMBL670709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Tissue |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.76 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.38 |
| CHEMBL2111781 | — | — | 1 | 8.73 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 8.62 |
| CHEMBL119687 | — | — | 1 | 8.44 |
| CHEMBL121274 | — | — | 1 | 8.44 |
| CHEMBL120512 | — | — | 1 | 8.40 |
| CHEMBL118889 | — | — | 1 | 8.35 |
| CHEMBL333955 | — | — | 1 | 8.13 |
| CHEMBL2111783 | — | — | 2 | 8.03 |
| CHEMBL116542 | — | — | 1 | 8.00 |
| CHEMBL118919 | — | — | 1 | 7.88 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.74 |
| CHEMBL333455 | — | — | 1 | 7.74 |
| CHEMBL64875 | — | — | 1 | 7.68 |
| CHEMBL2111782 | — | — | 2 | 7.64 |
| CHEMBL332600 | — | — | 1 | 7.61 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.41 |
| CHEMBL118092 | — | — | 1 | 7.24 |
| CHEMBL333246 | — | — | 1 | 6.99 |
| CHEMBL368324 | — | — | 1 | 6.96 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.4169 | nM | 9.38 |
| CHEMBL2111781 | — | Ki | = | 1.862 | nM | 8.73 |
| CHEMBL64249 | CLOROTEPINE | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL121274 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL119687 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL120512 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL118889 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL333955 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL2111783 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL116542 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL118919 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL333455 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL64875 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL2111782 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL332600 | — | Ki | = | 24.55 | nM | 7.61 |
| CHEMBL715 | OLANZAPINE | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL118092 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL333246 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL368324 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL42 | CLOZAPINE | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL2111783 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL2111782 | — | Ki | = | 851.14 | nM | 6.07 |