Assay Detail
Functional
CHEMBL774074
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Ability to stimulate peripheral prejunctional dopaminergic receptors by 50% inhibition of vasoconstrictor response to field stimulation in isolated perfused rabbit ear artery
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Syntheses and in vitro evaluation of 4-(2-aminoethyl)-2(3H)-indolones and related compounds as peripheral prejunctional dopamine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.99 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL587 | SKF-89124A | — | 1 | 8.70 |
| CHEMBL174011 | — | — | 1 | 7.75 |
| CHEMBL172846 | — | — | 1 | 7.55 |
| CHEMBL366579 | — | — | 1 | 7.28 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 7.14 |
| CHEMBL176858 | — | — | 1 | 7.10 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 7.00 |
| CHEMBL278188 | — | — | 1 | 6.94 |
| CHEMBL367076 | — | — | 1 | 6.66 |
| CHEMBL39845 | — | — | 1 | 6.16 |
| CHEMBL173227 | — | — | 1 | 6.12 |
| CHEMBL368590 | — | — | 1 | 5.52 |
| CHEMBL353386 | — | — | 1 | - |
| CHEMBL173979 | — | — | 1 | - |
| CHEMBL170703 | — | — | 1 | - |
| CHEMBL173855 | — | — | 1 | - |
| CHEMBL172980 | — | — | 1 | - |
| CHEMBL369274 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL587 | SKF-89124A | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL174011 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL172846 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL366579 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL59 | DOPAMINE | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL176858 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL589 | ROPINIROLE | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL278188 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL367076 | — | EC50 | = | 218.0 | nM | 6.66 |
| CHEMBL39845 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL173227 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL368590 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL353386 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL173979 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL170703 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL173855 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL172980 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL369274 | — | EC50 | > | 10000.0 | nM | - |