Assay Detail
Functional
CHEMBL964513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit rho-1 (CHEMBL3561) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 5.17 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33086 | t-4-AMINOCROTONIC ACID (TACA) | — | 1 | 6.40 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 6.10 |
| CHEMBL273481 | MUSCIMOL | 1.0 | 1 | 5.85 |
| CHEMBL507316 | — | — | 1 | 5.05 |
| CHEMBL446969 | — | — | 1 | 4.40 |
| CHEMBL488308 | — | — | 1 | 4.23 |
| CHEMBL32307 | — | — | 1 | 4.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33086 | t-4-AMINOCROTONIC ACID (TACA) | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL507316 | — | EC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL446969 | — | EC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL488308 | — | EC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL32307 | — | EC50 | = | 74000.0 | nM | 4.13 |