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Assay Detail

CHEMBL1040741

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

Binding
Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake
27
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Goodwin NC, Mabon R, Harrison BA, Shadoan MK, Almstead ZY, Xie Y, Healy J, Buhring LM, DaCosta CM, Bardenhagen J, Mseeh F, Liu Q, Nouraldeen A, Wilson AG, Kimball SD, Powell DR, Rawlins DB.
J Med Chem (2009) 52 : 6201 -6204
PubMed 19785435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.70 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569434 4 7.85
CHEMBL568164 1 7.50
CHEMBL585876 2 7.48
CHEMBL569903 1 7.44
CHEMBL567743 1 7.44
CHEMBL567953 1 7.35
CHEMBL585703 1 7.26
CHEMBL566471 1 7.24
CHEMBL567572 1 7.00
CHEMBL566076 1 6.82
CHEMBL566484 1 6.77
CHEMBL577519 1 6.75
CHEMBL567372 1 6.55
CHEMBL583016 1 6.23
CHEMBL566940 1 6.22
CHEMBL567778 1 6.21
CHEMBL568609 1 6.13
CHEMBL568398 1 5.96
CHEMBL567373 1 5.62
CHEMBL567954 1 5.44
CHEMBL567777 1 5.34
CHEMBL576252 1 -
CHEMBL582979 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569434 IC50 = 14.0 nM 7.85
CHEMBL569434 IC50 = 25.0 nM 7.60
CHEMBL569434 IC50 = 25.0 nM 7.60
CHEMBL568164 IC50 = 32.0 nM 7.50
CHEMBL585876 IC50 = 33.0 nM 7.48
CHEMBL567743 IC50 = 36.0 nM 7.44
CHEMBL569903 IC50 = 36.0 nM 7.44
CHEMBL567953 IC50 = 45.0 nM 7.35
CHEMBL585703 IC50 = 55.0 nM 7.26
CHEMBL566471 IC50 = 58.0 nM 7.24
CHEMBL567572 IC50 = 100.0 nM 7.00
CHEMBL566076 IC50 = 150.0 nM 6.82
CHEMBL566484 IC50 = 170.0 nM 6.77
CHEMBL577519 IC50 = 180.0 nM 6.75
CHEMBL567372 IC50 = 280.0 nM 6.55
CHEMBL585876 IC50 = 420.0 nM 6.38
CHEMBL583016 IC50 = 590.0 nM 6.23
CHEMBL566940 IC50 = 600.0 nM 6.22
CHEMBL567778 IC50 = 620.0 nM 6.21
CHEMBL568609 IC50 = 740.0 nM 6.13
CHEMBL568398 IC50 = 1100.0 nM 5.96
CHEMBL567373 IC50 = 2400.0 nM 5.62
CHEMBL567954 IC50 = 3600.0 nM 5.44
CHEMBL567777 IC50 = 4600.0 nM 5.34
CHEMBL569434 IC50 = 4800.0 nM 5.32
CHEMBL576252 IC50 > 30000.0 nM -
CHEMBL582979 IC50 > 30000.0 nM -