Assay Detail
Functional
CHEMBL1679247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
7
Total Activities
5
Compounds Tested
2
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 Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.77 | 5.65 |
| Kb | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397209 | — | — | 2 | 5.65 |
| CHEMBL1672299 | — | — | 1 | 4.70 |
| CHEMBL1672301 | — | — | 2 | 4.53 |
| CHEMBL112797 | SGS-742 | 2.0 | 1 | 4.21 |
| CHEMBL446306 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397209 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL1672299 | — | IC50 | = | 19910.0 | nM | 4.70 |
| CHEMBL1672301 | — | IC50 | = | 29740.0 | nM | 4.53 |
| CHEMBL112797 | SGS-742 | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL397209 | — | Kb | = | 2100.0 | nM | - |
| CHEMBL446306 | — | Kb | = | 2100.0 | nM | - |
| CHEMBL1672301 | — | Kb | = | 10000.0 | nM | - |