Assay Detail
Functional
CHEMBL618436
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonism of the 5-HT-3 receptor determined by inhibition of 5-HT-induced depolarization of the isolated rat vagus nerve.
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel antagonists of the 5-HT3 receptor. Synthesis and structure-activity relationships of (2-alkoxybenzoyl)ureas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 30 | 7.93 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL37239 | — | — | 1 | 9.20 |
| CHEMBL18041 | ZACOPRIDE | 2.0 | 1 | 9.10 |
| CHEMBL289115 | — | — | 1 | 8.90 |
| CHEMBL39479 | — | — | 1 | 8.90 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 8.70 |
| CHEMBL544002 | — | — | 1 | 8.70 |
| CHEMBL36157 | — | — | 1 | 8.69 |
| CHEMBL544244 | — | — | 1 | 8.60 |
| CHEMBL39621 | — | — | 1 | 8.50 |
| CHEMBL39934 | — | — | 1 | 8.20 |
| CHEMBL2114412 | — | — | 1 | 8.15 |
| CHEMBL37307 | — | — | 1 | 8.00 |
| CHEMBL543769 | — | — | 1 | 7.90 |
| CHEMBL2107804 | BEMESETRON | 2.0 | 1 | 7.80 |
| CHEMBL411467 | — | — | 1 | 7.77 |
| CHEMBL542090 | — | — | 1 | 7.50 |
| CHEMBL37419 | — | — | 1 | 7.44 |
| CHEMBL431499 | — | — | 1 | 7.40 |
| CHEMBL544952 | — | — | 1 | 7.33 |
| CHEMBL3350309 | — | — | 1 | 7.25 |
| CHEMBL544944 | — | — | 1 | 7.10 |
| CHEMBL286676 | — | — | 1 | 6.90 |
| CHEMBL555557 | — | — | 1 | 6.80 |
| CHEMBL544476 | — | — | 1 | 6.70 |
| CHEMBL37257 | — | — | 1 | 6.60 |
| CHEMBL36552 | — | — | 1 | - |
| CHEMBL288430 | — | — | 1 | - |
| CHEMBL39426 | — | — | 1 | - |
| CHEMBL36796 | — | — | 1 | - |
| CHEMBL37416 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL37239 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL18041 | ZACOPRIDE | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL289115 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL39479 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL46 | ONDANSETRON | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL544002 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL36157 | — | Kd | = | 2.042 | nM | 8.69 |
| CHEMBL544244 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL39621 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL39934 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL2114412 | — | Kd | = | 7.079 | nM | 8.15 |
| CHEMBL37307 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL543769 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL2107804 | BEMESETRON | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL411467 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL542090 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL37419 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL431499 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL544952 | — | Kd | = | 46.77 | nM | 7.33 |
| CHEMBL3350309 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL544944 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL286676 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL555557 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL544476 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL37257 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL36552 | — | Kd | > | 316.23 | nM | - |
| CHEMBL288430 | — | Kd | > | 31.62 | nM | - |
| CHEMBL39426 | — | Kd | > | 316.23 | nM | - |
| CHEMBL36796 | — | Kd | > | 316.23 | nM | - |
| CHEMBL37416 | — | Kd | > | 100.0 | nM | - |