Assay Detail
Binding
CHEMBL4838586
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Inhibition of mouse GAT3 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis
32
Total Activities
32
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 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 | 32 | 4.98 | 5.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781266 | — | — | 1 | 5.61 |
| CHEMBL4860085 | — | — | 1 | 5.36 |
| CHEMBL4861574 | — | — | 1 | 5.32 |
| CHEMBL4852705 | — | — | 1 | 5.32 |
| CHEMBL75035 | — | — | 1 | 5.29 |
| CHEMBL4873878 | — | — | 1 | 5.29 |
| CHEMBL4860167 | — | — | 1 | 5.25 |
| CHEMBL2414176 | — | — | 1 | 5.14 |
| CHEMBL4859850 | — | — | 1 | 5.09 |
| CHEMBL4863244 | — | — | 1 | 5.05 |
| CHEMBL4854550 | — | — | 1 | 5.01 |
| CHEMBL3289575 | — | — | 1 | 5.00 |
| CHEMBL4849009 | — | — | 1 | 4.99 |
| CHEMBL4853082 | — | — | 1 | 4.95 |
| CHEMBL4862980 | — | — | 1 | 4.94 |
| CHEMBL4870735 | — | — | 1 | 4.91 |
| CHEMBL4866914 | — | — | 1 | 4.90 |
| CHEMBL4854996 | — | — | 1 | 4.90 |
| CHEMBL4868987 | — | — | 1 | 4.90 |
| CHEMBL4850155 | — | — | 1 | 4.87 |
| CHEMBL4870136 | — | — | 1 | 4.87 |
| CHEMBL4849048 | — | — | 1 | 4.87 |
| CHEMBL4856428 | — | — | 1 | 4.86 |
| CHEMBL4849966 | — | — | 1 | 4.84 |
| CHEMBL4874054 | — | — | 1 | 4.79 |
| CHEMBL4858459 | — | — | 1 | 4.78 |
| CHEMBL4851621 | — | — | 1 | 4.77 |
| CHEMBL4852519 | — | — | 1 | 4.75 |
| CHEMBL4851901 | — | — | 1 | 4.75 |
| CHEMBL4850610 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781266 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL4860085 | — | IC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL4861574 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL4852705 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL75035 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL4873878 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL4860167 | — | IC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL2414176 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4859850 | — | IC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL4863244 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL4854550 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3289575 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4849009 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL4853082 | — | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL4862980 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL4870735 | — | IC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL4866914 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4868987 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4854996 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4850155 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4870136 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4849048 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4856428 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL4849966 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL4874054 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL4858459 | — | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL4851621 | — | IC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL4852519 | — | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL4851901 | — | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL4850610 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4595698 | — | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL3403559 | — | IC50 | = | 933254.3 | nM | - |