Assay Detail
Binding
CHEMBL618142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards 5-hydroxytryptamine 3 receptor
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 6.43 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 9.35 |
| CHEMBL51118 | — | — | 1 | 9.04 |
| CHEMBL292725 | — | — | 1 | 8.99 |
| CHEMBL52772 | — | — | 1 | 8.93 |
| CHEMBL54720 | — | — | 1 | 8.85 |
| CHEMBL63790 | — | — | 1 | 8.59 |
| CHEMBL62274 | — | — | 1 | 8.58 |
| CHEMBL65710 | — | — | 1 | 8.34 |
| CHEMBL301765 | — | — | 1 | 7.92 |
| CHEMBL294368 | — | — | 1 | 7.78 |
| CHEMBL418678 | — | — | 1 | 7.67 |
| CHEMBL64948 | — | — | 1 | 7.22 |
| CHEMBL65736 | — | — | 1 | 7.22 |
| CHEMBL62911 | — | — | 1 | 6.90 |
| CHEMBL261977 | — | — | 1 | 6.70 |
| CHEMBL302225 | — | — | 1 | 6.62 |
| CHEMBL65974 | — | — | 1 | 6.09 |
| CHEMBL65413 | — | — | 1 | 5.93 |
| CHEMBL27403 | — | — | 1 | 5.88 |
| CHEMBL66307 | — | — | 1 | 5.86 |
| CHEMBL303986 | — | — | 1 | 5.83 |
| CHEMBL68390 | — | — | 1 | 5.80 |
| CHEMBL302431 | — | — | 1 | 5.64 |
| CHEMBL62445 | — | — | 1 | 5.61 |
| CHEMBL62902 | — | — | 1 | 5.53 |
| CHEMBL62612 | — | — | 1 | 5.44 |
| CHEMBL293879 | — | — | 1 | 5.39 |
| CHEMBL64727 | — | — | 1 | 5.38 |
| CHEMBL302447 | — | — | 1 | 5.17 |
| CHEMBL64903 | — | — | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18772 | QUIPAZINE | IC50 | = | 0.4467 | nM | 9.35 |
| CHEMBL51118 | — | IC50 | = | 0.912 | nM | 9.04 |
| CHEMBL292725 | — | IC50 | = | 1.023 | nM | 8.99 |
| CHEMBL52772 | — | IC50 | = | 1.175 | nM | 8.93 |
| CHEMBL54720 | — | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL63790 | — | IC50 | = | 2.57 | nM | 8.59 |
| CHEMBL62274 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL65710 | — | IC50 | = | 4.571 | nM | 8.34 |
| CHEMBL301765 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL294368 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL418678 | — | IC50 | = | 21.38 | nM | 7.67 |
| CHEMBL64948 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL65736 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL62911 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL261977 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL302225 | — | IC50 | = | 239.88 | nM | 6.62 |
| CHEMBL65974 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL65413 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL27403 | — | IC50 | = | 1318.26 | nM | 5.88 |
| CHEMBL66307 | — | IC50 | = | 1380.38 | nM | 5.86 |
| CHEMBL303986 | — | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL68390 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL302431 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL62445 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL62902 | — | IC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL62612 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL293879 | — | IC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL64727 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL302447 | — | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL64903 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL62366 | — | IC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL292293 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL65669 | — | IC50 | = | 21379.62 | nM | 4.67 |
| CHEMBL66408 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL63114 | — | IC50 | = | 72443.6 | nM | 4.14 |
| CHEMBL63845 | — | IC50 | = | 74131.02 | nM | 4.13 |
| CHEMBL63905 | — | IC50 | = | 97723.72 | nM | 4.01 |
| CHEMBL64559 | — | IC50 | = | 1737800.83 | nM | - |
| CHEMBL63713 | — | IC50 | = | 269153.48 | nM | - |
| CHEMBL66540 | — | IC50 | = | 588843.66 | nM | - |
| CHEMBL66310 | — | IC50 | = | 245470.89 | nM | - |
| CHEMBL65212 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63588 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63289 | — | IC50 | = | 204173.79 | nM | - |
| CHEMBL417570 | — | IC50 | = | 1047128.55 | nM | - |
| CHEMBL293219 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL302104 | — | IC50 | > | 100000.0 | nM | - |