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Assay Detail

CHEMBL5658132

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human GLUT2 expressed in CHO cells assessed as reduction in fructose 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 CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876.
Siebeneicher H, Cleve A, Rehwinkel H, Neuhaus R, Heisler I, Müller T, Bauser M, Buchmann B.
ChemMedChem (2016) 11 : 2261 -2271
PubMed 27552707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 4.74 5.67

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
CHEMBL5661921 1 5.67
CHEMBL411729 CYTOCHALASIN B 1 5.55
CHEMBL5661909 1 5.41
CHEMBL5661924 1 5.25
CHEMBL5661942 1 5.15
CHEMBL5661925 1 5.07
CHEMBL5661833 1 5.03
CHEMBL4448899 BAY-876 1 4.97
CHEMBL5661865 1 4.89
CHEMBL5661932 1 4.74
CHEMBL5661938 1 4.72
CHEMBL5661934 1 4.70
CHEMBL5661847 1 4.69
CHEMBL5661842 1 4.65
CHEMBL5661867 1 4.59
CHEMBL5661885 1 4.58
CHEMBL5661884 1 4.44
CHEMBL5661896 1 4.44
CHEMBL5661940 1 4.29
CHEMBL5661927 1 4.29
CHEMBL5661930 1 4.29
CHEMBL5661845 1 4.29
CHEMBL5661933 1 4.29
CHEMBL5661874 1 4.29
CHEMBL5661901 1 4.16
CHEMBL5661922 1 -
CHEMBL5661891 1 -
CHEMBL5661878 1 -
CHEMBL5661892 1 -
CHEMBL5661861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5661921 IC50 = 2150.0 nM 5.67
CHEMBL411729 CYTOCHALASIN B IC50 = 2800.0 nM 5.55
CHEMBL5661909 IC50 = 3940.0 nM 5.41
CHEMBL5661924 IC50 = 5630.0 nM 5.25
CHEMBL5661942 IC50 = 7110.0 nM 5.15
CHEMBL5661925 IC50 = 8500.0 nM 5.07
CHEMBL5661833 IC50 = 9280.0 nM 5.03
CHEMBL4448899 BAY-876 IC50 = 10800.0 nM 4.97
CHEMBL5661865 IC50 = 12800.0 nM 4.89
CHEMBL5661932 IC50 = 18400.0 nM 4.74
CHEMBL5661938 IC50 = 18900.0 nM 4.72
CHEMBL5661934 IC50 = 20200.0 nM 4.70
CHEMBL5661847 IC50 = 20500.0 nM 4.69
CHEMBL5661842 IC50 = 22200.0 nM 4.65
CHEMBL5661867 IC50 = 25600.0 nM 4.59
CHEMBL5661885 IC50 = 26400.0 nM 4.58
CHEMBL5661884 IC50 = 36100.0 nM 4.44
CHEMBL5661896 IC50 = 36100.0 nM 4.44
CHEMBL5661940 IC50 = 51200.0 nM 4.29
CHEMBL5661874 IC50 = 51200.0 nM 4.29
CHEMBL5661933 IC50 = 51200.0 nM 4.29
CHEMBL5661845 IC50 = 51200.0 nM 4.29
CHEMBL5661930 IC50 = 51200.0 nM 4.29
CHEMBL5661927 IC50 = 51200.0 nM 4.29
CHEMBL5661901 IC50 = 69000.0 nM 4.16
CHEMBL5661888 IC50 - -
CHEMBL5661915 IC50 - -
CHEMBL5661919 IC50 - -
CHEMBL5661873 IC50 - -
CHEMBL5661849 IC50 - -
CHEMBL5661939 IC50 - -
CHEMBL5661843 IC50 - -
CHEMBL5661853 IC50 - -
CHEMBL5661920 IC50 - -
CHEMBL5661852 IC50 - -
CHEMBL5661834 IC50 - -
CHEMBL5661890 IC50 - -
CHEMBL5661913 IC50 - -
CHEMBL4552180 BAY-588 IC50 > 10000.0 nM -
CHEMBL5661895 IC50 - -
CHEMBL5661908 IC50 - -
CHEMBL5661850 IC50 - -
CHEMBL5661836 IC50 - -
CHEMBL5661907 IC50 - -
CHEMBL5661929 IC50 - -
CHEMBL5661861 IC50 - -
CHEMBL5661892 IC50 - -
CHEMBL5661878 IC50 - -
CHEMBL5661891 IC50 - -
CHEMBL5661922 IC50 - -