Assay Detail
Binding
CHEMBL1775995
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Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.70 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164505 | — | — | 1 | 5.85 |
| CHEMBL1773934 | — | — | 1 | 4.66 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 4.56 |
| CHEMBL1773944 | — | — | 1 | 4.56 |
| CHEMBL75035 | — | — | 1 | 4.46 |
| CHEMBL1773947 | — | — | 1 | 4.12 |
| CHEMBL20724 | — | — | 1 | - |
| CHEMBL543494 | — | — | 1 | - |
| CHEMBL554597 | — | — | 1 | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 1 | - |
| CHEMBL84253 | — | — | 1 | - |
| CHEMBL1773945 | — | — | 1 | - |
| CHEMBL297390 | — | — | 1 | - |
| CHEMBL1773942 | — | — | 1 | - |
| CHEMBL1773937 | — | — | 1 | - |
| CHEMBL773 | GLYCINE | 4.0 | 1 | - |
| CHEMBL297569 | BETA-ALANINE | — | 1 | - |
| CHEMBL284116 | 5-AMINOVALERIC ACID | 1.0 | 1 | - |
| CHEMBL1773946 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164505 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1773934 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL1773944 | — | IC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL75035 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1773947 | — | IC50 | = | 75857.76 | nM | 4.12 |
| CHEMBL20724 | — | IC50 | = | 501187.23 | nM | - |
| CHEMBL543494 | — | IC50 | = | 223872.11 | nM | - |
| CHEMBL554597 | — | IC50 | = | 162181.01 | nM | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | IC50 | = | 102329.3 | nM | - |
| CHEMBL84253 | — | IC50 | = | 645654.23 | nM | - |
| CHEMBL1773945 | — | IC50 | = | 245470.89 | nM | - |
| CHEMBL297390 | — | IC50 | = | 199526.23 | nM | - |
| CHEMBL1773942 | — | IC50 | = | 630957.34 | nM | - |
| CHEMBL1773937 | — | IC50 | = | 524807.46 | nM | - |
| CHEMBL773 | GLYCINE | IC50 | = | 2238721.14 | nM | - |
| CHEMBL297569 | BETA-ALANINE | IC50 | = | 331131.12 | nM | - |
| CHEMBL284116 | 5-AMINOVALERIC ACID | IC50 | = | 134896.29 | nM | - |
| CHEMBL1773946 | — | IC50 | = | 380189.4 | nM | - |