Assay Detail
Binding
CHEMBL2388852
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Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Ileal sodium/bile acid cotransporter (CHEMBL2073686) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.75 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2387397 | — | — | 1 | 9.70 |
| CHEMBL2385105 | — | — | 1 | 9.05 |
| CHEMBL2387408 | LINERIXIBAT | 3.0 | 1 | 8.72 |
| CHEMBL2387399 | — | — | 1 | 8.64 |
| CHEMBL332370 | — | — | 1 | 7.66 |
| CHEMBL2387402 | — | — | 1 | - |
| CHEMBL2387419 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2387397 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2385105 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2387408 | LINERIXIBAT | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2387399 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL332370 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2387402 | — | IC50 | - | — | - | |
| CHEMBL2387419 | — | IC50 | - | — | - |