Assay Detail
Binding
CHEMBL617198
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Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin 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 | 4.86 | 5.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415933 | — | — | 1 | 5.79 |
| CHEMBL51118 | — | — | 1 | 5.63 |
| CHEMBL301765 | — | — | 1 | 5.58 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 5.46 |
| CHEMBL54720 | — | — | 1 | 5.36 |
| CHEMBL52612 | — | — | 1 | 5.13 |
| CHEMBL54914 | — | — | 1 | 5.10 |
| CHEMBL53416 | — | — | 1 | 4.98 |
| CHEMBL53490 | — | — | 1 | 4.84 |
| CHEMBL53573 | — | — | 1 | 4.82 |
| CHEMBL299524 | — | — | 1 | 4.77 |
| CHEMBL27403 | — | — | 1 | 4.73 |
| CHEMBL52867 | — | — | 1 | 4.70 |
| CHEMBL299097 | — | — | 1 | 4.67 |
| CHEMBL299231 | — | — | 1 | 4.60 |
| CHEMBL52772 | — | — | 1 | 4.42 |
| CHEMBL52625 | — | — | 1 | 4.36 |
| CHEMBL49932 | — | — | 1 | 4.34 |
| CHEMBL54125 | — | — | 1 | 4.33 |
| CHEMBL54246 | — | — | 1 | 4.29 |
| CHEMBL300725 | — | — | 1 | 4.15 |
| CHEMBL298649 | — | — | 1 | - |
| CHEMBL53195 | — | — | 1 | - |
| CHEMBL416662 | — | — | 1 | - |
| CHEMBL53662 | — | — | 1 | - |
| CHEMBL51225 | — | — | 1 | - |
| CHEMBL432897 | — | — | 1 | - |
| CHEMBL50740 | — | — | 1 | - |
| CHEMBL50456 | — | — | 1 | - |
| CHEMBL52007 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415933 | — | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL51118 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL301765 | — | IC50 | = | 2630.27 | nM | 5.58 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL54720 | — | IC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL52612 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL54914 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL53416 | — | IC50 | = | 10471.29 | nM | 4.98 |
| CHEMBL53490 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL53573 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL299524 | — | IC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL27403 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL52867 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL299097 | — | IC50 | = | 21379.62 | nM | 4.67 |
| CHEMBL299231 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL52772 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL52625 | — | IC50 | = | 43651.58 | nM | 4.36 |
| CHEMBL49932 | — | IC50 | = | 45708.82 | nM | 4.34 |
| CHEMBL54125 | — | IC50 | = | 46773.51 | nM | 4.33 |
| CHEMBL54246 | — | IC50 | = | 51286.14 | nM | 4.29 |
| CHEMBL300725 | — | IC50 | = | 70794.58 | nM | 4.15 |
| CHEMBL300692 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL51675 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL410531 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52800 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL299634 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52007 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL50456 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL50740 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL432897 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL51225 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53662 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL416662 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53195 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL298649 | — | IC50 | > | 100000.0 | nM | - |