Assay Detail
Binding
CHEMBL3386947
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Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent neutral amino acid transporter B(0)AT2 (CHEMBL3351189) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 4.92 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357043 | — | — | 1 | 5.47 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 5.40 |
| CHEMBL3357024 | — | — | 1 | 5.35 |
| CHEMBL3357033 | — | — | 1 | 5.34 |
| CHEMBL331603 | — | — | 1 | 5.31 |
| CHEMBL3357037 | — | — | 1 | 5.31 |
| CHEMBL3357041 | — | — | 1 | 5.30 |
| CHEMBL3357044 | — | — | 1 | 5.28 |
| CHEMBL3357029 | — | — | 1 | 5.28 |
| CHEMBL3357045 | — | — | 1 | 5.24 |
| CHEMBL3357049 | — | — | 1 | 5.11 |
| CHEMBL3357035 | — | — | 1 | 5.11 |
| CHEMBL3357042 | — | — | 1 | 4.97 |
| CHEMBL3357027 | — | — | 1 | 4.91 |
| CHEMBL3357028 | — | — | 1 | 4.83 |
| CHEMBL338697 | — | — | 1 | 4.79 |
| CHEMBL3357034 | — | — | 1 | 4.78 |
| CHEMBL3357023 | — | — | 1 | 4.75 |
| CHEMBL3357022 | — | — | 1 | 4.74 |
| CHEMBL3357047 | — | — | 1 | 4.73 |
| CHEMBL3357032 | — | — | 1 | 4.71 |
| CHEMBL316889 | — | — | 1 | 4.64 |
| CHEMBL3357046 | — | — | 1 | 4.58 |
| CHEMBL3357030 | — | — | 1 | 4.46 |
| CHEMBL116935 | — | — | 1 | 4.44 |
| CHEMBL3357048 | — | — | 1 | 4.41 |
| CHEMBL3357040 | — | — | 1 | 4.38 |
| CHEMBL10971 | SCH-37370 | — | 1 | 4.26 |
| CHEMBL3357031 | — | — | 1 | - |
| CHEMBL3357025 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357043 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL998 | LORATADINE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3357024 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3357033 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL331603 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3357037 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3357041 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3357044 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3357029 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3357045 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3357035 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3357049 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3357042 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL3357027 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL3357028 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL338697 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL3357034 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL3357023 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL3357022 | — | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL3357047 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL3357032 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL316889 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL3357046 | — | IC50 | = | 26400.0 | nM | 4.58 |
| CHEMBL3357030 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL116935 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL3357048 | — | IC50 | = | 39100.0 | nM | 4.41 |
| CHEMBL3357040 | — | IC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL10971 | SCH-37370 | IC50 | = | 54800.0 | nM | 4.26 |
| CHEMBL3357039 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357038 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357036 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL91397 | RUPATADINE | IC50 | > | 40000.0 | nM | - |
| CHEMBL1172 | DESLORATADINE | IC50 | = | 172000.0 | nM | - |
| CHEMBL420316 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357026 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357021 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357025 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL3357031 | — | IC50 | > | 80000.0 | nM | - |