Assay Detail
Binding
CHEMBL4398053
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Inhibition of human GAT2 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 2 (CHEMBL4535) ↗| 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 | 4.96 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4458674 | — | — | 2 | 5.54 |
| CHEMBL1788265 | — | — | 2 | 5.14 |
| CHEMBL79325 | — | — | 2 | 5.10 |
| CHEMBL349005 | — | — | 2 | 4.80 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 4.58 |
| CHEMBL4526098 | — | — | 2 | - |
| CHEMBL4471977 | — | — | 1 | - |
| CHEMBL4586460 | — | — | 1 | - |
| CHEMBL4455221 | — | — | 1 | - |
| CHEMBL4442696 | — | — | 1 | - |
| CHEMBL4464494 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4458674 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4458674 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1788265 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL79325 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL1788265 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL349005 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL349005 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL79325 | — | IC50 | = | 79100.0 | nM | 4.10 |
| CHEMBL4442696 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464494 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464494 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4455221 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4586460 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4471977 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4526098 | — | IC50 | = | 125892.54 | nM | - |
| CHEMBL4526098 | — | IC50 | = | 132200.0 | nM | - |