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Assay Detail

CHEMBL1005353

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

Binding
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/glucose cotransporter 2 (CHEMBL3884)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of fluorescent SGLT2 inhibitors.
Lansdell MI, Burring DJ, Hepworth D, Strawbridge M, Graham E, Guyot T, Betson MS, Hart JD.
Bioorg Med Chem Lett (2008) 18 : 4944 -4947
PubMed 18755586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.48 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496138 1 7.92
CHEMBL497971 1 7.48
CHEMBL521565 1 7.35
CHEMBL447975 1 7.26
CHEMBL449080 1 7.02
CHEMBL500268 1 6.99
CHEMBL448655 1 6.91
CHEMBL499912 1 6.91
CHEMBL452214 1 6.88
CHEMBL500780 1 6.84
CHEMBL504484 1 6.83
CHEMBL445964 1 6.81
CHEMBL444227 1 6.81
CHEMBL511083 1 6.69
CHEMBL508623 1 6.69
CHEMBL506354 1 6.57
CHEMBL501165 1 6.54
CHEMBL509911 1 6.50
CHEMBL443616 1 6.46
CHEMBL503496 1 6.43
CHEMBL442864 1 6.38
CHEMBL473046 1 6.37
CHEMBL496518 1 6.30
CHEMBL245067 PHLORIZIN 1 6.12
CHEMBL449778 1 6.08
CHEMBL171648 1 6.07
CHEMBL509278 1 5.80
CHEMBL508141 1 5.70
CHEMBL500899 1 5.62
CHEMBL457594 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496138 IC50 = 12.0 nM 7.92
CHEMBL497971 IC50 = 33.0 nM 7.48
CHEMBL521565 IC50 = 45.0 nM 7.35
CHEMBL447975 IC50 = 55.0 nM 7.26
CHEMBL449080 IC50 = 95.0 nM 7.02
CHEMBL500268 IC50 = 102.0 nM 6.99
CHEMBL448655 IC50 = 123.0 nM 6.91
CHEMBL499912 IC50 = 122.0 nM 6.91
CHEMBL452214 IC50 = 131.0 nM 6.88
CHEMBL500780 IC50 = 145.0 nM 6.84
CHEMBL504484 IC50 = 148.0 nM 6.83
CHEMBL445964 IC50 = 154.0 nM 6.81
CHEMBL444227 IC50 = 155.0 nM 6.81
CHEMBL511083 IC50 = 205.0 nM 6.69
CHEMBL508623 IC50 = 203.0 nM 6.69
CHEMBL506354 IC50 = 267.0 nM 6.57
CHEMBL501165 IC50 = 286.0 nM 6.54
CHEMBL509911 IC50 = 315.0 nM 6.50
CHEMBL443616 IC50 = 350.0 nM 6.46
CHEMBL503496 IC50 = 370.0 nM 6.43
CHEMBL442864 IC50 = 420.0 nM 6.38
CHEMBL473046 IC50 = 430.0 nM 6.37
CHEMBL496518 IC50 = 495.0 nM 6.30
CHEMBL245067 PHLORIZIN IC50 = 752.0 nM 6.12
CHEMBL449778 IC50 = 835.0 nM 6.08
CHEMBL171648 IC50 = 850.0 nM 6.07
CHEMBL509278 IC50 = 1570.0 nM 5.80
CHEMBL508141 IC50 = 2000.0 nM 5.70
CHEMBL500899 IC50 = 2400.0 nM 5.62
CHEMBL457594 IC50 = 8000.0 nM 5.10
CHEMBL445247 IC50 = 11000.0 nM 4.96
CHEMBL466749 IC50 = 15050.0 nM 4.82