Assay Detail
Binding
CHEMBL5658131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GLUT1 expressed in human DLD-1 cells assessed as reduction in glucose uptake by measuring decrease in ATP production incubated for 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay
64
Total Activities
64
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | DLD-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Solute carrier family 2, facilitated glucose transporter member 1 (CHEMBL2535) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 7.70 | 9.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5661873 | — | — | 1 | 9.52 |
| CHEMBL5661842 | — | — | 1 | 9.00 |
| CHEMBL5661847 | — | — | 1 | 9.00 |
| CHEMBL5661848 | — | — | 1 | 9.00 |
| CHEMBL5661910 | — | — | 1 | 8.70 |
| CHEMBL5661896 | — | — | 1 | 8.70 |
| CHEMBL4448899 | BAY-876 | — | 1 | 8.70 |
| CHEMBL5661838 | — | — | 1 | 8.52 |
| CHEMBL5661843 | — | — | 1 | 8.52 |
| CHEMBL5661878 | — | — | 1 | 8.52 |
| CHEMBL5661888 | — | — | 1 | 8.52 |
| CHEMBL5661885 | — | — | 1 | 8.52 |
| CHEMBL5661934 | — | — | 1 | 8.40 |
| CHEMBL5661828 | — | — | 1 | 8.40 |
| CHEMBL5661865 | — | — | 1 | 8.40 |
| CHEMBL5661849 | — | — | 1 | 8.30 |
| CHEMBL5661852 | — | — | 1 | 8.30 |
| CHEMBL5661921 | — | — | 1 | 8.30 |
| CHEMBL5661908 | — | — | 1 | 8.30 |
| CHEMBL5661901 | — | — | 1 | 8.22 |
| CHEMBL5661932 | — | — | 1 | 8.22 |
| CHEMBL5661940 | — | — | 1 | 8.15 |
| CHEMBL5661884 | — | — | 1 | 8.15 |
| CHEMBL5661918 | — | — | 1 | 8.15 |
| CHEMBL5661892 | — | — | 1 | 8.15 |
| CHEMBL5661930 | — | — | 1 | 8.15 |
| CHEMBL5661915 | — | — | 1 | 8.10 |
| CHEMBL5661919 | — | — | 1 | 8.10 |
| CHEMBL5661850 | — | — | 1 | 8.05 |
| CHEMBL5661933 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5661873 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5661842 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661847 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661848 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661910 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5661896 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4448899 | BAY-876 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5661843 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5661878 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5661888 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5661838 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5661885 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5661934 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5661828 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5661865 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5661849 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5661908 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5661921 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5661852 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5661901 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5661932 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5661930 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5661892 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5661884 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5661940 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5661918 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5661915 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5661919 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5661850 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5661933 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5661907 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5661913 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5661874 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5661939 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5661911 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5661922 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5661833 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5661929 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5661834 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5661890 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5661859 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5661942 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5661845 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5661925 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5661895 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5661862 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5661920 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5661927 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5661924 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5661867 | — | IC50 | = | 89.0 | nM | 7.05 |