Assay Detail
Binding
CHEMBL4767588
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Inhibition of mouse GAT4 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method
37
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
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 4.98 | 5.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.81 |
| CHEMBL4126078 | — | — | 1 | 5.78 |
| CHEMBL4793917 | — | — | 2 | 5.41 |
| CHEMBL4798809 | — | — | 1 | 5.30 |
| CHEMBL4788344 | — | — | 2 | 5.26 |
| CHEMBL4780692 | — | — | 1 | 5.25 |
| CHEMBL4794776 | — | — | 1 | 5.24 |
| CHEMBL4781266 | — | — | 1 | 5.21 |
| CHEMBL4792403 | — | — | 1 | 5.18 |
| CHEMBL4796172 | — | — | 1 | 5.16 |
| CHEMBL4786927 | — | — | 1 | 5.15 |
| CHEMBL4784962 | — | — | 1 | 5.13 |
| CHEMBL4798908 | — | — | 1 | 5.12 |
| CHEMBL4785506 | — | — | 1 | 5.09 |
| CHEMBL4793317 | — | — | 1 | 5.06 |
| CHEMBL4777433 | — | — | 1 | 5.02 |
| CHEMBL4778208 | — | — | 2 | 5.02 |
| CHEMBL4787407 | — | — | 1 | 5.02 |
| CHEMBL4795098 | — | — | 1 | 4.99 |
| CHEMBL4791625 | — | — | 1 | 4.96 |
| CHEMBL4787828 | — | — | 2 | 4.88 |
| CHEMBL4778862 | — | — | 1 | 4.86 |
| CHEMBL4778326 | — | — | 1 | 4.79 |
| CHEMBL4787408 | — | — | 1 | 4.77 |
| CHEMBL4791461 | — | — | 1 | 4.77 |
| CHEMBL4778176 | — | — | 2 | 4.75 |
| CHEMBL4778497 | — | — | 1 | 4.68 |
| CHEMBL4782298 | — | — | 1 | 4.48 |
| CHEMBL4796143 | — | — | 1 | 4.11 |
| CHEMBL4595698 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL4126078 | — | IC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL4793917 | — | IC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL4798809 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4788344 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL4780692 | — | IC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL4794776 | — | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL4781266 | — | IC50 | = | 6165.95 | nM | 5.21 |
| CHEMBL4792403 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL4796172 | — | IC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL4788344 | — | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL4786927 | — | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL4784962 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL4798908 | — | IC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL4785506 | — | IC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL4793317 | — | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL4777433 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL4787407 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL4778208 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL4778208 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL4795098 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL4791625 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL4787828 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL4778862 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL4778326 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL4787408 | — | IC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL4791461 | — | IC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL4778176 | — | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL4793917 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL4778497 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL4787828 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL4778176 | — | IC50 | = | 29512.09 | nM | 4.53 |
| CHEMBL4782298 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL4796143 | — | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL4595698 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL473104 | — | IC50 | = | 851138.04 | nM | - |
| CHEMBL4787153 | — | IC50 | > | 301995.17 | nM | - |