Assay Detail
Binding
CHEMBL616558
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Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
5-hydroxytryptamine receptor 1B (CHEMBL3459) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.06 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | — | 1 | 8.80 |
| CHEMBL15933 | — | — | 1 | 8.68 |
| CHEMBL276928 | — | — | 1 | 7.64 |
| CHEMBL15855 | — | — | 1 | 7.30 |
| CHEMBL15961 | — | — | 1 | 7.30 |
| CHEMBL16035 | — | — | 1 | 7.20 |
| CHEMBL15837 | — | — | 1 | 7.11 |
| CHEMBL278917 | — | — | 1 | 7.10 |
| CHEMBL2079627 | — | — | 1 | 7.07 |
| CHEMBL274922 | — | — | 1 | 6.95 |
| CHEMBL280000 | — | — | 1 | 6.92 |
| CHEMBL279320 | — | — | 1 | 6.88 |
| CHEMBL15965 | — | — | 1 | 6.65 |
| CHEMBL279646 | — | — | 1 | 6.63 |
| CHEMBL430122 | — | — | 1 | 6.57 |
| CHEMBL15909 | — | — | 1 | 6.52 |
| CHEMBL15139 | — | — | 1 | 6.33 |
| CHEMBL15808 | — | — | 1 | 6.25 |
| CHEMBL280314 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL15933 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL276928 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL15855 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL15961 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL16035 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL15837 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL278917 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2079627 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL274922 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL280000 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL279320 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL15965 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL279646 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL430122 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL15909 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL15139 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL15808 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL280314 | — | IC50 | = | 633.0 | nM | 6.20 |