Assay Detail
Binding
CHEMBL619423
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro by displacement of [3H]LY-278584 from 5-hydroxytryptamine 3 receptor on rat entorhinal cortex
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.45 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294083 | — | — | 1 | 9.50 |
| CHEMBL62692 | — | — | 1 | 9.50 |
| CHEMBL63025 | — | — | 1 | 9.50 |
| CHEMBL294109 | — | — | 1 | 9.40 |
| CHEMBL56900 | LERISETRON | 3.0 | 1 | 9.20 |
| CHEMBL59689 | — | — | 1 | 9.00 |
| CHEMBL60102 | — | — | 1 | 8.80 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 8.80 |
| CHEMBL294522 | — | — | 1 | 8.80 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 8.70 |
| CHEMBL64880 | — | — | 1 | 8.70 |
| CHEMBL64489 | — | — | 1 | 8.50 |
| CHEMBL64801 | — | — | 1 | 8.40 |
| CHEMBL60103 | — | — | 1 | 8.00 |
| CHEMBL292066 | — | — | 1 | 7.50 |
| CHEMBL62270 | — | — | 1 | 7.30 |
| CHEMBL62778 | — | — | 1 | 7.20 |
| CHEMBL64782 | — | — | 1 | 7.10 |
| CHEMBL64060 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294083 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL62692 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL63025 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL294109 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL56900 | LERISETRON | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL59689 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL60102 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL56564 | TROPISETRON | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL294522 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL289469 | GRANISETRON | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL64880 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL64489 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL64801 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL60103 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL292066 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL62270 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL62778 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL64782 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL64060 | — | Ki | = | 199.53 | nM | 6.70 |