Assay Detail
Binding
CHEMBL5145826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at 5-HT3 receptor in guinea-pig ileum assessed as inhibition of 5HT-induced contraction
15
Total Activities
15
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel D<sub>2</sub>/5-HT receptor modulators related to cariprazine with potential implication to schizophrenia treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.91 | 6.52 |
| Kd | 2 | 7.60 | 7.80 |
| Ki | 1 | 8.40 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 8.40 |
| CHEMBL4228145 | — | — | 1 | 7.80 |
| CHEMBL184379 | — | — | 1 | 7.40 |
| CHEMBL5190788 | — | — | 1 | 6.52 |
| CHEMBL5205697 | — | — | 1 | 6.00 |
| CHEMBL5200023 | — | — | 1 | 6.00 |
| CHEMBL5193798 | — | — | 1 | 5.52 |
| CHEMBL5209381 | — | — | 1 | 5.52 |
| CHEMBL5176374 | — | — | 1 | - |
| CHEMBL5173624 | — | — | 1 | - |
| CHEMBL5195091 | — | — | 1 | - |
| CHEMBL5196828 | — | — | 1 | - |
| CHEMBL5172819 | — | — | 1 | - |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289469 | GRANISETRON | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4228145 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL184379 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL5190788 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5205697 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5200023 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5193798 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5209381 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5176374 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5173624 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5195091 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5196828 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5172819 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | = | 630000.0 | nM | - |
| CHEMBL42 | CLOZAPINE | IC50 | = | 110000.0 | nM | - |