Assay Detail
Binding
CHEMBL5658133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GLUT3 expressed in human GLUT1-/- 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
62
Total Activities
62
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 3 (CHEMBL5215) ↗| 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 | 5.46 | 7.46 |
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 |
|---|---|---|---|---|
| CHEMBL5661838 | — | — | 1 | 7.46 |
| CHEMBL5661939 | — | — | 1 | 7.07 |
| CHEMBL5661873 | — | — | 1 | 6.96 |
| CHEMBL411729 | CYTOCHALASIN B | — | 1 | 6.92 |
| CHEMBL5661843 | — | — | 1 | 6.64 |
| CHEMBL5661849 | — | — | 1 | 6.54 |
| CHEMBL5661845 | — | — | 1 | 6.52 |
| CHEMBL5661918 | — | — | 1 | 6.34 |
| CHEMBL5661842 | — | — | 1 | 6.33 |
| CHEMBL5661848 | — | — | 1 | 6.26 |
| CHEMBL5661901 | — | — | 1 | 6.24 |
| CHEMBL5661921 | — | — | 1 | 6.21 |
| CHEMBL5661888 | — | — | 1 | 6.12 |
| CHEMBL5661852 | — | — | 1 | 5.96 |
| CHEMBL5661874 | — | — | 1 | 5.92 |
| CHEMBL5661844 | — | — | 1 | 5.81 |
| CHEMBL4448899 | BAY-876 | — | 1 | 5.78 |
| CHEMBL5661915 | — | — | 1 | 5.78 |
| CHEMBL5661885 | — | — | 1 | 5.76 |
| CHEMBL5661862 | — | — | 1 | 5.70 |
| CHEMBL5661828 | — | — | 1 | 5.69 |
| CHEMBL5661924 | — | — | 1 | 5.62 |
| CHEMBL5661833 | — | — | 1 | 5.61 |
| CHEMBL5661896 | — | — | 1 | 5.56 |
| CHEMBL5661834 | — | — | 1 | 5.54 |
| CHEMBL5661934 | — | — | 1 | 5.54 |
| CHEMBL5661847 | — | — | 1 | 5.54 |
| CHEMBL5661913 | — | — | 1 | 5.54 |
| CHEMBL5661919 | — | — | 1 | 5.54 |
| CHEMBL5661929 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5661838 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5661939 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5661873 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL411729 | CYTOCHALASIN B | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5661843 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5661849 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5661845 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5661918 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5661842 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5661848 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5661901 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5661921 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5661888 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5661852 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL5661874 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5661844 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4448899 | BAY-876 | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL5661915 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL5661885 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL5661862 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL5661828 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL5661924 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL5661833 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL5661896 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL5661919 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL5661934 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL5661913 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL5661834 | — | IC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL5661847 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL5661929 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL5661908 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL5661884 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL5661895 | — | IC50 | = | 4320.0 | nM | 5.37 |
| CHEMBL5661861 | — | IC50 | = | 4980.0 | nM | 5.30 |
| CHEMBL5661920 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4552180 | BAY-588 | IC50 | = | 5470.0 | nM | 5.26 |
| CHEMBL5661853 | — | IC50 | = | 5650.0 | nM | 5.25 |
| CHEMBL5661878 | — | IC50 | = | 5950.0 | nM | 5.22 |
| CHEMBL5661910 | — | IC50 | = | 6070.0 | nM | 5.22 |
| CHEMBL5661942 | — | IC50 | = | 6090.0 | nM | 5.21 |
| CHEMBL5661850 | — | IC50 | = | 6550.0 | nM | 5.18 |
| CHEMBL5661911 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL5661841 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL5661867 | — | IC50 | = | 9090.0 | nM | 5.04 |
| CHEMBL5661890 | — | IC50 | = | 9890.0 | nM | 5.00 |
| CHEMBL5661840 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL5661892 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL5661865 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL5661907 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL5661925 | — | IC50 | = | 15600.0 | nM | 4.81 |