Assay Detail
Binding
CHEMBL616188
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Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
5-hydroxytryptamine receptor 1B (CHEMBL3459) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.14 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301765 | — | — | 1 | 7.86 |
| CHEMBL53490 | — | — | 1 | 6.82 |
| CHEMBL299231 | — | — | 1 | 6.69 |
| CHEMBL54914 | — | — | 1 | 6.61 |
| CHEMBL27403 | — | — | 1 | 6.47 |
| CHEMBL51118 | — | — | 1 | 6.38 |
| CHEMBL54720 | — | — | 1 | 5.99 |
| CHEMBL415933 | — | — | 1 | 5.45 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 5.15 |
| CHEMBL300692 | — | — | 1 | 5.00 |
| CHEMBL53416 | — | — | 1 | 4.89 |
| CHEMBL53573 | — | — | 1 | 4.88 |
| CHEMBL416662 | — | — | 1 | 4.84 |
| CHEMBL299634 | — | — | 1 | 4.72 |
| CHEMBL299097 | — | — | 1 | 4.71 |
| CHEMBL52612 | — | — | 1 | 4.58 |
| CHEMBL299524 | — | — | 1 | 4.50 |
| CHEMBL54125 | — | — | 1 | 4.42 |
| CHEMBL54246 | — | — | 1 | 4.36 |
| CHEMBL49932 | — | — | 1 | 4.31 |
| CHEMBL52625 | — | — | 1 | 4.25 |
| CHEMBL52867 | — | — | 1 | 4.23 |
| CHEMBL53662 | — | — | 1 | 4.16 |
| CHEMBL298649 | — | — | 1 | 4.15 |
| CHEMBL50456 | — | — | 1 | 4.11 |
| CHEMBL50740 | — | — | 1 | 4.01 |
| CHEMBL51225 | — | — | 1 | - |
| CHEMBL432897 | — | — | 1 | - |
| CHEMBL52007 | — | — | 1 | - |
| CHEMBL53195 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301765 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL53490 | — | IC50 | = | 151.36 | nM | 6.82 |
| CHEMBL299231 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL54914 | — | IC50 | = | 245.47 | nM | 6.61 |
| CHEMBL27403 | — | IC50 | = | 338.84 | nM | 6.47 |
| CHEMBL51118 | — | IC50 | = | 416.87 | nM | 6.38 |
| CHEMBL54720 | — | IC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL415933 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL300692 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL53416 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL53573 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL416662 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL299634 | — | IC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL299097 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL52612 | — | IC50 | = | 26302.68 | nM | 4.58 |
| CHEMBL299524 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL54125 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL54246 | — | IC50 | = | 43651.58 | nM | 4.36 |
| CHEMBL49932 | — | IC50 | = | 48977.88 | nM | 4.31 |
| CHEMBL52625 | — | IC50 | = | 56234.13 | nM | 4.25 |
| CHEMBL52867 | — | IC50 | = | 58884.37 | nM | 4.23 |
| CHEMBL53662 | — | IC50 | = | 69183.1 | nM | 4.16 |
| CHEMBL298649 | — | IC50 | = | 70794.58 | nM | 4.15 |
| CHEMBL50456 | — | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL50740 | — | IC50 | = | 97723.72 | nM | 4.01 |
| CHEMBL51675 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL410531 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52772 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL300725 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52800 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53195 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52007 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL432897 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL51225 | — | IC50 | > | 100000.0 | nM | - |