Assay Detail
Binding
CHEMBL652040
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against uptake of [14C]taurocholate in baby hamster kidney cells transfected with cDNA from human Apical Sodium-Codependent Bile Acid Transporter
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | kidney |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Ileal sodium/bile acid cotransporter (CHEMBL2778) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.97 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332974 | — | — | 1 | 8.80 |
| CHEMBL332973 | — | — | 1 | 8.52 |
| CHEMBL122498 | — | — | 1 | 8.22 |
| CHEMBL341104 | — | — | 1 | 8.10 |
| CHEMBL340291 | — | — | 1 | 7.66 |
| CHEMBL125997 | — | — | 1 | 7.58 |
| CHEMBL341082 | — | — | 1 | 7.46 |
| CHEMBL122745 | — | — | 1 | 7.36 |
| CHEMBL332370 | — | — | 1 | 7.32 |
| CHEMBL122229 | — | — | 1 | 7.08 |
| CHEMBL434814 | — | — | 1 | 6.70 |
| CHEMBL331910 | — | — | 1 | 6.51 |
| CHEMBL331015 | — | — | 1 | 6.50 |
| CHEMBL331631 | — | — | 1 | 6.50 |
| CHEMBL123319 | — | — | 1 | 6.24 |
| CHEMBL124715 | — | — | 1 | 6.24 |
| CHEMBL123444 | — | — | 1 | 6.16 |
| CHEMBL124239 | — | — | 1 | 6.01 |
| CHEMBL331235 | — | — | 1 | 5.92 |
| CHEMBL123542 | — | — | 1 | 5.92 |
| CHEMBL332606 | — | — | 1 | 5.60 |
| CHEMBL333922 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332974 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL332973 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL122498 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL341104 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL340291 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL125997 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL341082 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL122745 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL332370 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL122229 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL434814 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL331910 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL331015 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL331631 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL123319 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL124715 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL123444 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL124239 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL331235 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL123542 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL332606 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL333922 | — | IC50 | > | 1000.0 | nM | - |