Assay Detail
Binding
CHEMBL617709
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Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor from rat cortical homogenate using [3H]zacopride as radioligand
43
Total Activities
43
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
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 7.65 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139327 | — | — | 1 | 9.17 |
| CHEMBL136978 | — | — | 1 | 9.10 |
| CHEMBL341474 | — | — | 1 | 9.09 |
| CHEMBL54914 | — | — | 1 | 9.00 |
| CHEMBL342690 | — | — | 1 | 8.95 |
| CHEMBL136090 | — | — | 1 | 8.80 |
| CHEMBL137621 | — | — | 1 | 8.66 |
| CHEMBL53573 | — | — | 1 | 8.64 |
| CHEMBL136449 | — | — | 1 | 8.59 |
| CHEMBL137565 | — | — | 1 | 8.51 |
| CHEMBL337101 | — | — | 1 | 8.44 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 8.42 |
| CHEMBL136525 | — | — | 1 | 8.42 |
| CHEMBL136524 | — | — | 1 | 8.28 |
| CHEMBL335803 | — | — | 1 | 8.18 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 8.17 |
| CHEMBL136108 | — | — | 1 | 8.09 |
| CHEMBL136536 | — | — | 1 | 8.06 |
| CHEMBL337324 | — | — | 1 | 7.96 |
| CHEMBL137564 | — | — | 1 | 7.92 |
| CHEMBL342447 | — | — | 1 | 7.89 |
| CHEMBL136979 | — | — | 1 | 7.79 |
| CHEMBL422279 | — | — | 1 | 7.75 |
| CHEMBL138849 | — | — | 1 | 7.66 |
| CHEMBL343919 | — | — | 1 | 7.62 |
| CHEMBL134473 | — | — | 1 | 7.52 |
| CHEMBL140295 | — | — | 1 | 7.42 |
| CHEMBL136416 | — | — | 1 | 7.36 |
| CHEMBL423719 | — | — | 1 | 7.22 |
| CHEMBL2107804 | BEMESETRON | 2.0 | 1 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139327 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL136978 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL341474 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL54914 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL342690 | — | IC50 | = | 1.13 | nM | 8.95 |
| CHEMBL136090 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL137621 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL53573 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL136449 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL137565 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL337101 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL136525 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL136524 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL335803 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL46 | ONDANSETRON | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL136108 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL136536 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL337324 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL137564 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL342447 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL136979 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL422279 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL138849 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL343919 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL134473 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL140295 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL136416 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL423719 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2107804 | BEMESETRON | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL136772 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL136138 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL342381 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL139534 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL139271 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL424662 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL136266 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL138034 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL334462 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL136666 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL134970 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL424471 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL336699 | — | IC50 | = | 3800.0 | nM | 5.42 |