Assay Detail
Binding
CHEMBL4838580
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Inhibition of mouse GAT1 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis
35
Total Activities
35
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 |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 4.90 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4595698 | — | — | 1 | 8.27 |
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.88 |
| CHEMBL69064 | — | — | 1 | 5.70 |
| CHEMBL4852705 | — | — | 1 | 5.20 |
| CHEMBL4873878 | — | — | 1 | 5.20 |
| CHEMBL4859850 | — | — | 1 | 5.18 |
| CHEMBL4861574 | — | — | 1 | 5.14 |
| CHEMBL4854550 | — | — | 1 | 5.09 |
| CHEMBL4781266 | — | — | 1 | 5.06 |
| CHEMBL4856428 | — | — | 1 | 5.00 |
| CHEMBL3289575 | — | — | 1 | 4.89 |
| CHEMBL303402 | — | — | 1 | 4.87 |
| CHEMBL4860167 | — | — | 1 | 4.86 |
| CHEMBL4853082 | — | — | 1 | 4.86 |
| CHEMBL4854996 | — | — | 1 | 4.85 |
| CHEMBL2414176 | — | — | 1 | 4.72 |
| CHEMBL4862980 | — | — | 1 | 4.70 |
| CHEMBL4863244 | — | — | 1 | 4.68 |
| CHEMBL4858459 | — | — | 1 | 4.66 |
| CHEMBL4849048 | — | — | 1 | 4.66 |
| CHEMBL4870735 | — | — | 1 | 4.66 |
| CHEMBL4868987 | — | — | 1 | 4.62 |
| CHEMBL4866914 | — | — | 1 | 4.60 |
| CHEMBL4851621 | — | — | 1 | 4.56 |
| CHEMBL4849966 | — | — | 1 | 4.55 |
| CHEMBL4851901 | — | — | 1 | 4.54 |
| CHEMBL4852519 | — | — | 1 | 4.54 |
| CHEMBL4850610 | — | — | 1 | 4.50 |
| CHEMBL4874054 | — | — | 1 | 4.48 |
| CHEMBL4870136 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4595698 | — | IC50 | = | 5.37 | nM | 8.27 |
| CHEMBL1027 | TIAGABINE | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL69064 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4852705 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4873878 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4859850 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL4861574 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4854550 | — | IC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL4781266 | — | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL4856428 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3289575 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL303402 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4860167 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL4853082 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL4854996 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL2414176 | — | IC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL4862980 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4863244 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL4849048 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL4870735 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL4858459 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL4868987 | — | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL4866914 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4851621 | — | IC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL4849966 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL4852519 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL4851901 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL4850610 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4874054 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL4870136 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL4849009 | — | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL4850155 | — | IC50 | = | 69183.1 | nM | 4.16 |
| CHEMBL4860085 | — | IC50 | = | 72443.6 | nM | 4.14 |
| CHEMBL75035 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL3403559 | — | IC50 | = | 562341.33 | nM | - |