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Assay Detail

CHEMBL1680964

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 after 2 hrs by liquid scintillation counting
ChEMBL ↗
47
Total Activities
47
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

Synthesis and SAR of Thiazolylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors.
Song KS, Lee SH, Kim MJ, Seo HJ, Lee J, Lee SH, Jung ME, Son EJ, Lee M, Kim J, Lee J.
ACS Med Chem Lett (2011) 2 : 182 -187
PubMed 24900297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 8.05 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 9.31
CHEMBL1642509 — — 1 9.14
CHEMBL1672796 — — 1 9.11
CHEMBL1672817 — — 1 8.96
CHEMBL1672795 — — 1 8.94
CHEMBL1672803 — — 1 8.89
CHEMBL1672814 — — 1 8.85
CHEMBL1672802 — — 1 8.85
CHEMBL1672794 — — 1 8.80
CHEMBL1672804 — — 1 8.72
CHEMBL1672816 — — 1 8.55
CHEMBL1672798 — — 1 8.50
CHEMBL1672815 — — 1 8.35
CHEMBL1672779 — — 1 8.33
CHEMBL1672776 — — 1 8.30
CHEMBL1672806 — — 1 8.21
CHEMBL1672805 — — 1 8.20
CHEMBL1672807 — — 1 8.13
CHEMBL1672786 — — 1 8.09
CHEMBL1672793 — — 1 8.03
CHEMBL1672808 — — 1 8.01
CHEMBL1672781 — — 1 8.01
CHEMBL1672780 — — 1 7.94
CHEMBL1672777 — — 1 7.91
CHEMBL1672784 — — 1 7.91
CHEMBL1672791 — — 1 7.88
CHEMBL1672797 — — 1 7.88
CHEMBL1672775 — — 1 7.88
CHEMBL1672799 — — 1 7.85
CHEMBL1672809 — — 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429910 DAPAGLIFLOZIN IC50 = 0.49 nM 9.31
CHEMBL1642509 — IC50 = 0.72 nM 9.14
CHEMBL1672796 — IC50 = 0.772 nM 9.11
CHEMBL1672817 — IC50 = 1.11 nM 8.96
CHEMBL1672795 — IC50 = 1.14 nM 8.94
CHEMBL1672803 — IC50 = 1.28 nM 8.89
CHEMBL1672814 — IC50 = 1.42 nM 8.85
CHEMBL1672802 — IC50 = 1.43 nM 8.85
CHEMBL1672794 — IC50 = 1.57 nM 8.80
CHEMBL1672804 — IC50 = 1.89 nM 8.72
CHEMBL1672816 — IC50 = 2.79 nM 8.55
CHEMBL1672798 — IC50 = 3.13 nM 8.50
CHEMBL1672815 — IC50 = 4.47 nM 8.35
CHEMBL1672779 — IC50 = 4.69 nM 8.33
CHEMBL1672776 — IC50 = 5.0 nM 8.30
CHEMBL1672806 — IC50 = 6.11 nM 8.21
CHEMBL1672805 — IC50 = 6.36 nM 8.20
CHEMBL1672807 — IC50 = 7.36 nM 8.13
CHEMBL1672786 — IC50 = 8.2 nM 8.09
CHEMBL1672793 — IC50 = 9.31 nM 8.03
CHEMBL1672808 — IC50 = 9.73 nM 8.01
CHEMBL1672781 — IC50 = 9.71 nM 8.01
CHEMBL1672780 — IC50 = 11.5 nM 7.94
CHEMBL1672777 — IC50 = 12.4 nM 7.91
CHEMBL1672784 — IC50 = 12.4 nM 7.91
CHEMBL1672791 — IC50 = 13.3 nM 7.88
CHEMBL1672797 — IC50 = 13.3 nM 7.88
CHEMBL1672775 — IC50 = 13.3 nM 7.88
CHEMBL1672799 — IC50 = 14.0 nM 7.85
CHEMBL1672809 — IC50 = 14.6 nM 7.84
CHEMBL1672773 — IC50 = 16.7 nM 7.78
CHEMBL1672783 — IC50 = 18.8 nM 7.73
CHEMBL1672790 — IC50 = 18.9 nM 7.72
CHEMBL1672785 — IC50 = 19.6 nM 7.71
CHEMBL1672792 — IC50 = 21.2 nM 7.67
CHEMBL1672810 — IC50 = 22.6 nM 7.65
CHEMBL1672782 — IC50 = 25.4 nM 7.59
CHEMBL1672787 — IC50 = 30.9 nM 7.51
CHEMBL1672811 — IC50 = 36.7 nM 7.43
CHEMBL1672800 — IC50 = 50.3 nM 7.30
CHEMBL1672778 — IC50 = 51.4 nM 7.29
CHEMBL1672813 — IC50 = 54.8 nM 7.26
CHEMBL1672788 — IC50 = 56.4 nM 7.25
CHEMBL1672789 — IC50 = 58.7 nM 7.23
CHEMBL1672774 — IC50 = 119.0 nM 6.92
CHEMBL1672812 — IC50 = 140.0 nM 6.85
CHEMBL1672801 — IC50 > 10000.0 nM -