Assay Detail
Binding
CHEMBL617854
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Binding affinity against 5-Hydroxytryptamine 2C Receptor was measured using [3H]N-methyl-mesulergine 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 |
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 | 5.49 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301765 | — | — | 1 | 7.46 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 7.21 |
| CHEMBL53490 | — | — | 1 | 6.57 |
| CHEMBL54914 | — | — | 1 | 6.56 |
| CHEMBL299231 | — | — | 1 | 6.43 |
| CHEMBL51118 | — | — | 1 | 6.12 |
| CHEMBL53573 | — | — | 1 | 5.76 |
| CHEMBL54720 | — | — | 1 | 5.73 |
| CHEMBL53416 | — | — | 1 | 5.61 |
| CHEMBL52625 | — | — | 1 | 5.28 |
| CHEMBL299634 | — | — | 1 | 5.28 |
| CHEMBL415933 | — | — | 1 | 5.13 |
| CHEMBL299524 | — | — | 1 | 4.97 |
| CHEMBL49932 | — | — | 1 | 4.87 |
| CHEMBL54125 | — | — | 1 | 4.86 |
| CHEMBL52612 | — | — | 1 | 4.86 |
| CHEMBL299097 | — | — | 1 | 4.44 |
| CHEMBL432897 | — | — | 1 | 4.35 |
| CHEMBL54246 | — | — | 1 | 4.24 |
| CHEMBL27403 | — | — | 1 | 4.01 |
| CHEMBL298649 | — | — | 1 | - |
| CHEMBL300725 | — | — | 1 | - |
| CHEMBL53195 | — | — | 1 | - |
| CHEMBL52772 | — | — | 1 | - |
| CHEMBL416662 | — | — | 1 | - |
| CHEMBL53662 | — | — | 1 | - |
| CHEMBL52867 | — | — | 1 | - |
| CHEMBL51225 | — | — | 1 | - |
| CHEMBL50740 | — | — | 1 | - |
| CHEMBL50456 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301765 | — | IC50 | = | 34.67 | nM | 7.46 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 61.66 | nM | 7.21 |
| CHEMBL53490 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL54914 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL299231 | — | IC50 | = | 371.54 | nM | 6.43 |
| CHEMBL51118 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL53573 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL54720 | — | IC50 | = | 1862.09 | nM | 5.73 |
| CHEMBL53416 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL52625 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL299634 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL415933 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL299524 | — | IC50 | = | 10715.19 | nM | 4.97 |
| CHEMBL49932 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL52612 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL54125 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL299097 | — | IC50 | = | 36307.81 | nM | 4.44 |
| CHEMBL432897 | — | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL54246 | — | IC50 | = | 57543.99 | nM | 4.24 |
| CHEMBL27403 | — | IC50 | = | 97723.72 | nM | 4.01 |
| CHEMBL300692 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL51675 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL410531 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52800 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52007 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL50456 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL50740 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL51225 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52867 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53662 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL416662 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52772 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53195 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL300725 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL298649 | — | IC50 | > | 100000.0 | nM | - |