Assay Detail
Binding
CHEMBL4398052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT1 expressed in Flp-In CHO cells assessed as reduction in [3H]GABA uptake incubated for 3 mins by liquid scintillation counting method
17
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL1903) ↗| 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 |
|---|---|---|---|
| IC50 | 17 | 4.80 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1788265 | — | — | 2 | 5.60 |
| CHEMBL349005 | — | — | 2 | 5.50 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.00 |
| CHEMBL4458674 | — | — | 2 | 4.15 |
| CHEMBL4526098 | — | — | 2 | 4.01 |
| CHEMBL79325 | — | — | 2 | - |
| CHEMBL4471977 | — | — | 1 | - |
| CHEMBL4586460 | — | — | 1 | - |
| CHEMBL4455221 | — | — | 1 | - |
| CHEMBL4442696 | — | — | 1 | - |
| CHEMBL4464494 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1788265 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL349005 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1788265 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL349005 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4458674 | — | IC50 | = | 71400.0 | nM | 4.15 |
| CHEMBL4458674 | — | IC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL4526098 | — | IC50 | = | 96900.0 | nM | 4.01 |
| CHEMBL4526098 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4471977 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4586460 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4455221 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4442696 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464494 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464494 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL79325 | — | IC50 | = | 178800.0 | nM | - |
| CHEMBL79325 | — | IC50 | = | 158489.32 | nM | - |