Assay Detail
Binding
CHEMBL873476
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Binding affinity towards 5-hydroxytryptamine 2A receptor
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 5.10 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261977 | — | — | 1 | 6.07 |
| CHEMBL62274 | — | — | 1 | 6.07 |
| CHEMBL65736 | — | — | 1 | 6.03 |
| CHEMBL64948 | — | — | 1 | 5.97 |
| CHEMBL65974 | — | — | 1 | 5.89 |
| CHEMBL68390 | — | — | 1 | 5.75 |
| CHEMBL51118 | — | — | 1 | 5.63 |
| CHEMBL302225 | — | — | 1 | 5.63 |
| CHEMBL301765 | — | — | 1 | 5.58 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 5.46 |
| CHEMBL54720 | — | — | 1 | 5.36 |
| CHEMBL63713 | — | — | 1 | 5.29 |
| CHEMBL62366 | — | — | 1 | 5.13 |
| CHEMBL294368 | — | — | 1 | 5.13 |
| CHEMBL63790 | — | — | 1 | 4.96 |
| CHEMBL65669 | — | — | 1 | 4.86 |
| CHEMBL64903 | — | — | 1 | 4.86 |
| CHEMBL303986 | — | — | 1 | 4.84 |
| CHEMBL302431 | — | — | 1 | 4.76 |
| CHEMBL62911 | — | — | 1 | 4.76 |
| CHEMBL27403 | — | — | 1 | 4.73 |
| CHEMBL65710 | — | — | 1 | 4.71 |
| CHEMBL418678 | — | — | 1 | 4.65 |
| CHEMBL292725 | — | — | 1 | 4.61 |
| CHEMBL52772 | — | — | 1 | 4.42 |
| CHEMBL292293 | — | — | 1 | 4.40 |
| CHEMBL302447 | — | — | 1 | 4.20 |
| CHEMBL293879 | — | — | 1 | 4.15 |
| CHEMBL62902 | — | — | 1 | 4.06 |
| CHEMBL66540 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261977 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL62274 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL65736 | — | IC50 | = | 933.25 | nM | 6.03 |
| CHEMBL64948 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL65974 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL68390 | — | IC50 | = | 1778.28 | nM | 5.75 |
| CHEMBL51118 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL302225 | — | 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 |
| CHEMBL63713 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL294368 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL62366 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL63790 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL65669 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL64903 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL303986 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL302431 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL62911 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL27403 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL65710 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL418678 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL292725 | — | IC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL52772 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL292293 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL302447 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL293879 | — | IC50 | = | 70794.58 | nM | 4.15 |
| CHEMBL62902 | — | IC50 | = | 87096.36 | nM | 4.06 |
| CHEMBL62445 | — | IC50 | = | 301995.17 | nM | - |
| CHEMBL66307 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL302104 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL293219 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL417570 | — | IC50 | = | 151356.12 | nM | - |
| CHEMBL63289 | — | IC50 | = | 123026.88 | nM | - |
| CHEMBL62612 | — | IC50 | = | 173780.08 | nM | - |
| CHEMBL63845 | — | IC50 | = | 831763.77 | nM | - |
| CHEMBL64727 | — | IC50 | = | 478630.09 | nM | - |
| CHEMBL63588 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63905 | — | IC50 | = | 446683.59 | nM | - |
| CHEMBL66408 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63114 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL66310 | — | IC50 | = | 371535.23 | nM | - |
| CHEMBL65212 | — | IC50 | = | 112201.85 | nM | - |
| CHEMBL64559 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL65413 | — | IC50 | = | 190546.07 | nM | - |
| CHEMBL66540 | — | IC50 | = | 338844.16 | nM | - |