Assay Detail
Binding
CHEMBL4031697
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Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method
41
Total Activities
33
Compounds Tested
2
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 betaine transporter (CHEMBL3715) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 4.38 | 4.87 |
| Ki | 2 | 4.60 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1882801 | — | — | 2 | 4.87 |
| CHEMBL228972 | — | — | 1 | 4.82 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 4.75 |
| CHEMBL4060376 | — | — | 2 | 4.39 |
| CHEMBL4068983 | — | — | 1 | 4.38 |
| CHEMBL123282 | — | — | 2 | 4.04 |
| CHEMBL4080696 | — | — | 2 | 4.00 |
| CHEMBL4101561 | — | — | 1 | - |
| CHEMBL4075865 | — | — | 1 | - |
| CHEMBL4079046 | — | — | 1 | - |
| CHEMBL4090080 | — | — | 1 | - |
| CHEMBL4070660 | — | — | 1 | - |
| CHEMBL4097791 | — | — | 1 | - |
| CHEMBL4091409 | — | — | 1 | - |
| CHEMBL4069676 | — | — | 1 | - |
| CHEMBL4102978 | — | — | 1 | - |
| CHEMBL4072002 | — | — | 1 | - |
| CHEMBL4075412 | — | — | 1 | - |
| CHEMBL4063054 | — | — | 1 | - |
| CHEMBL4071982 | — | — | 1 | - |
| CHEMBL4072046 | — | — | 1 | - |
| CHEMBL4097124 | — | — | 1 | - |
| CHEMBL4070193 | — | — | 1 | - |
| CHEMBL4089518 | — | — | 1 | - |
| CHEMBL1603838 | — | — | 2 | - |
| CHEMBL1710951 | — | — | 2 | - |
| CHEMBL4078727 | — | — | 2 | - |
| CHEMBL4072452 | — | — | 1 | - |
| CHEMBL4066152 | — | — | 1 | - |
| CHEMBL4069761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1882801 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL228972 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL1882801 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4060376 | — | IC50 | = | 40738.03 | nM | 4.39 |
| CHEMBL4068983 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL4060376 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL123282 | — | IC50 | = | 91201.08 | nM | 4.04 |
| CHEMBL123282 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL4080696 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4080696 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4076258 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4071982 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4075865 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4075412 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4072002 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4102978 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4072452 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4091409 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4097791 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4070660 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4090080 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4079046 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4069761 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4063054 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4077212 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4075423 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4101561 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4069676 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4066152 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4078727 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL4078727 | — | IC50 | = | 169824.37 | nM | - |
| CHEMBL1710951 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL1710951 | — | IC50 | = | 181970.09 | nM | - |
| CHEMBL1603838 | — | IC50 | = | 290000.0 | nM | - |
| CHEMBL1603838 | — | IC50 | = | 295120.92 | nM | - |
| CHEMBL4089518 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4070193 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4072046 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4097124 | — | IC50 | > | 50000.0 | nM | - |