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Assay Detail

CHEMBL977366

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 intracellular accumulation of [14C]alpha-methyl glucopyranoside
16
Total Activities
16
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

Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Ellsworth BA, Meng W, Patel M, Girotra RN, Wu G, Sher PM, Hagan DL, Obermeier MT, Humphreys WG, Robertson JG, Wang A, Han S, Waldron TL, Morgan NN, Whaley JM, Washburn WN.
Bioorg Med Chem Lett (2008) 18 : 4770 -4773
PubMed 18707880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.58 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447016 1 8.10
CHEMBL488696 1 7.66
CHEMBL245067 PHLORIZIN 1 7.46
CHEMBL486461 1 7.16
CHEMBL486670 1 6.72
CHEMBL487667 1 6.54
CHEMBL486637 1 6.37
CHEMBL520379 1 6.32
CHEMBL486664 1 6.29
CHEMBL488839 1 6.27
CHEMBL486837 1 6.21
CHEMBL507895 1 6.20
CHEMBL520894 1 6.15
CHEMBL486636 1 6.01
CHEMBL487650 1 5.92
CHEMBL487666 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447016 EC50 = 8.0 nM 8.10
CHEMBL488696 EC50 = 22.0 nM 7.66
CHEMBL245067 PHLORIZIN EC50 = 35.0 nM 7.46
CHEMBL486461 EC50 = 69.0 nM 7.16
CHEMBL486670 EC50 = 190.0 nM 6.72
CHEMBL487667 EC50 = 290.0 nM 6.54
CHEMBL486637 EC50 = 430.0 nM 6.37
CHEMBL520379 EC50 = 480.0 nM 6.32
CHEMBL486664 EC50 = 510.0 nM 6.29
CHEMBL488839 EC50 = 540.0 nM 6.27
CHEMBL486837 EC50 = 623.0 nM 6.21
CHEMBL507895 EC50 = 630.0 nM 6.20
CHEMBL520894 EC50 = 710.0 nM 6.15
CHEMBL486636 EC50 = 970.0 nM 6.01
CHEMBL487650 EC50 = 1200.0 nM 5.92
CHEMBL487666 EC50 = 1200.0 nM 5.92