Assay Detail
Binding
CHEMBL5658134
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay
62
Total Activities
62
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Solute carrier family 2, facilitated glucose transporter member 4 (CHEMBL5874) ↗| 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 | 62 | 6.39 | 7.89 |
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 | 7.89 |
| CHEMBL5661852 | — | — | 1 | 7.80 |
| CHEMBL5661842 | — | — | 1 | 7.80 |
| CHEMBL5661939 | — | — | 1 | 7.77 |
| CHEMBL5661888 | — | — | 1 | 7.54 |
| CHEMBL5661849 | — | — | 1 | 7.36 |
| CHEMBL5661933 | — | — | 1 | 7.21 |
| CHEMBL5661878 | — | — | 1 | 7.06 |
| CHEMBL5661828 | — | — | 1 | 7.05 |
| CHEMBL5661843 | — | — | 1 | 7.03 |
| CHEMBL5661915 | — | — | 1 | 7.02 |
| CHEMBL5661884 | — | — | 1 | 6.92 |
| CHEMBL5661913 | — | — | 1 | 6.80 |
| CHEMBL5661901 | — | — | 1 | 6.77 |
| CHEMBL5661910 | — | — | 1 | 6.75 |
| CHEMBL5661921 | — | — | 1 | 6.72 |
| CHEMBL5661932 | — | — | 1 | 6.66 |
| CHEMBL5661859 | — | — | 1 | 6.55 |
| CHEMBL411729 | CYTOCHALASIN B | — | 1 | 6.55 |
| CHEMBL4448899 | BAY-876 | — | 1 | 6.54 |
| CHEMBL5661924 | — | — | 1 | 6.47 |
| CHEMBL5661938 | — | — | 1 | 6.44 |
| CHEMBL5661847 | — | — | 1 | 6.43 |
| CHEMBL5661908 | — | — | 1 | 6.43 |
| CHEMBL5661874 | — | — | 1 | 6.42 |
| CHEMBL5661838 | — | — | 1 | 6.40 |
| CHEMBL5661911 | — | — | 1 | 6.39 |
| CHEMBL5661918 | — | — | 1 | 6.38 |
| CHEMBL4552180 | BAY-588 | — | 1 | 6.30 |
| CHEMBL5661930 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5661873 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5661852 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5661842 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5661939 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5661888 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5661849 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5661933 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5661878 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5661828 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5661843 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5661915 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5661884 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5661913 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5661901 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5661910 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5661921 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5661932 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5661859 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL411729 | CYTOCHALASIN B | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4448899 | BAY-876 | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5661924 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5661938 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5661847 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5661908 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5661874 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5661838 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5661911 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5661918 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4552180 | BAY-588 | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5661930 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5661934 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5661907 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5661848 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5661919 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL5661895 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5661844 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5661850 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5661929 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5661845 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5661836 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL5661902 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL5661892 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL5661834 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL5661867 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL5661833 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL5661840 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL5661942 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5661896 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5661861 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL5661862 | — | IC50 | = | 2050.0 | nM | 5.69 |