Assay Detail
Functional
CHEMBL982104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at serotonin 5HT2A receptor assessed as effect on 5HT-induced isometric contractile force in isolated rings of pig coronary artery
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Sus scrofa |
| Tissue | Coronary artery |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 8.54 | 9.19 |
| pD2 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201170 | — | — | 1 | 9.19 |
| CHEMBL203637 | — | — | 1 | 9.05 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.88 |
| CHEMBL201525 | — | — | 1 | 8.70 |
| CHEMBL380330 | — | — | 1 | 8.69 |
| CHEMBL231070 | — | — | 1 | 8.67 |
| CHEMBL276778 | — | — | 1 | 8.47 |
| CHEMBL216439 | — | — | 1 | 8.42 |
| CHEMBL508399 | — | — | 1 | 8.40 |
| CHEMBL389357 | — | — | 1 | 8.24 |
| CHEMBL459871 | — | — | 1 | 7.21 |
| CHEMBL441618 | — | — | 1 | - |
| CHEMBL245570 | — | — | 1 | - |
| CHEMBL216258 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201170 | — | Kd | = | 0.6457 | nM | 9.19 |
| CHEMBL203637 | — | Kd | = | 0.8913 | nM | 9.05 |
| CHEMBL51 | KETANSERIN | Kd | = | 1.318 | nM | 8.88 |
| CHEMBL201525 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL380330 | — | Kd | = | 2.042 | nM | 8.69 |
| CHEMBL231070 | — | Kd | = | 2.138 | nM | 8.67 |
| CHEMBL276778 | — | Kd | = | 3.388 | nM | 8.47 |
| CHEMBL216439 | — | Kd | = | 3.802 | nM | 8.42 |
| CHEMBL508399 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL389357 | — | Kd | = | 5.754 | nM | 8.24 |
| CHEMBL459871 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL441618 | — | pD2 | = | 9.79 | — | - |
| CHEMBL245570 | — | pD2 | = | 9.97 | — | - |
| CHEMBL216258 | — | pD2 | = | 9.77 | — | - |