Assay Detail
Binding
CHEMBL4398028
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Agonist activity at recombinant human GABA-A rho-1 receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay
28
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 5.51 | 6.47 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.47 |
| CHEMBL4464494 | — | — | 4 | 5.92 |
| CHEMBL4442696 | — | — | 2 | 5.80 |
| CHEMBL4458674 | — | — | 2 | 5.56 |
| CHEMBL4554798 | — | — | 2 | 5.43 |
| CHEMBL4526098 | — | — | 2 | 5.42 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 2 | 5.34 |
| CHEMBL4547372 | — | — | 2 | 5.27 |
| CHEMBL79325 | — | — | 2 | 5.19 |
| CHEMBL1788265 | — | — | 2 | 5.08 |
| CHEMBL4471977 | — | — | 2 | - |
| CHEMBL349005 | — | — | 2 | - |
| CHEMBL71460 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 338.84 | nM | 6.47 |
| CHEMBL4464494 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4464494 | — | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL4442696 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4442696 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4458674 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL4458674 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4554798 | — | EC50 | = | 3715.35 | nM | 5.43 |
| CHEMBL4554798 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4526098 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4526098 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | EC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL4547372 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4547372 | — | EC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL79325 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL79325 | — | EC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL4464494 | — | EC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL4464494 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL1788265 | — | EC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL1788265 | — | EC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL71460 | — | EC50 | - | — | - | |
| CHEMBL349005 | — | EC50 | - | — | - | |
| CHEMBL4471977 | — | EC50 | - | — | - | |
| CHEMBL71460 | — | pEC50 | - | — | - | |
| CHEMBL349005 | — | pEC50 | - | — | - | |
| CHEMBL4471977 | — | pEC50 | - | — | - |