Assay Detail
Binding
CHEMBL618129
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Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | NG 108-15 |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094132) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 60 | 6.62 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 8.70 |
| CHEMBL288591 | — | — | 1 | 8.52 |
| CHEMBL43078 | — | — | 1 | 7.92 |
| CHEMBL45773 | — | — | 1 | 7.82 |
| CHEMBL13790 | — | — | 1 | 7.77 |
| CHEMBL40567 | — | — | 1 | 7.60 |
| CHEMBL278509 | — | — | 1 | 7.50 |
| CHEMBL13823 | — | — | 1 | 7.46 |
| CHEMBL337213 | — | — | 1 | 7.42 |
| CHEMBL61778 | — | — | 1 | 7.40 |
| CHEMBL43798 | — | — | 1 | 7.40 |
| CHEMBL336522 | — | — | 1 | 7.32 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.21 |
| CHEMBL42752 | — | — | 1 | 7.21 |
| CHEMBL335877 | — | — | 1 | 6.90 |
| CHEMBL131053 | — | — | 1 | 6.82 |
| CHEMBL277120 | — | — | 1 | 6.76 |
| CHEMBL41853 | — | — | 1 | 6.72 |
| CHEMBL840 | 4-CHLOROPHENYLBIGUANIDE | — | 1 | 6.70 |
| CHEMBL42538 | — | — | 1 | 6.66 |
| CHEMBL40190 | — | — | 1 | 6.65 |
| CHEMBL129150 | — | — | 1 | 6.61 |
| CHEMBL41040 | — | — | 1 | 6.50 |
| CHEMBL128275 | — | — | 1 | 6.25 |
| CHEMBL128567 | — | — | 1 | 6.18 |
| CHEMBL289319 | — | — | 1 | 6.11 |
| CHEMBL131570 | — | — | 1 | 5.92 |
| CHEMBL13791 | PHENYL BIGUANIDE | — | 1 | 5.92 |
| CHEMBL40488 | — | — | 1 | 5.92 |
| CHEMBL40459 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18772 | QUIPAZINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL288591 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL43078 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL45773 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL13790 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL40567 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL278509 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL13823 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL337213 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL61778 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL43798 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL336522 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL42752 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL335877 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL131053 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL277120 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL41853 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL840 | 4-CHLOROPHENYLBIGUANIDE | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL42538 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL40190 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL129150 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL41040 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL128275 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL128567 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL289319 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL13791 | PHENYL BIGUANIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL40488 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL131570 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL40459 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL274866 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL128659 | — | Ki | = | 1450.0 | nM | 5.84 |
| CHEMBL43459 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL59517 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL114478 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL14047 | PHENYLGUANIDINE | Ki | = | 2340.0 | nM | 5.63 |
| CHEMBL9666 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL419966 | PYRAXININE | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL9434 | PHENYLPIPERAZINE | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL44236 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL295000 | — | Ki | = | 6520.0 | nM | 5.19 |
| CHEMBL131145 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL130703 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL131289 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL335754 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL131771 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL20969 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL274497 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL336107 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL130698 | — | Ki | > | 10000.0 | nM | - |