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Assay Detail

CHEMBL1781790

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Binding
Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting
ChEMBL ↗
53
Total Activities
33
Compounds Tested
2
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

Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors.
Du X, Lizarzaburu M, Turcotte S, Lee T, Greenberg J, Shan B, Fan P, Ling Y, Medina JC, Houze J.
Bioorg Med Chem Lett (2011) 21 : 3774 -3779
PubMed 21565497 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.51 8.52
Inhibition 20 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779340 — — 1 8.52
CHEMBL1779217 — — 2 8.52
CHEMBL429910 DAPAGLIFLOZIN 4.0 1 8.52
CHEMBL1779339 — — 1 8.40
CHEMBL1779345 — — 1 8.30
CHEMBL1779338 — — 1 8.30
CHEMBL1779336 — — 1 8.15
CHEMBL1779223 — — 1 8.15
CHEMBL1779343 — — 1 8.10
CHEMBL1779214 — — 2 8.10
CHEMBL1779218 — — 2 8.00
CHEMBL1779344 — — 1 8.00
CHEMBL1762505 — — 2 8.00
CHEMBL1779219 — — 2 7.92
CHEMBL1779341 — — 1 7.92
CHEMBL1779216 — — 2 7.89
CHEMBL1779221 — — 2 7.89
CHEMBL1779220 — — 2 7.85
CHEMBL1779207 — — 2 7.68
CHEMBL1779208 — — 2 7.66
CHEMBL1779215 — — 2 7.64
CHEMBL1779205 — — 2 7.44
CHEMBL1779222 — — 1 7.39
CHEMBL1779203 — — 2 7.24
CHEMBL1779209 — — 2 7.23
CHEMBL1779213 — — 2 7.14
CHEMBL1779211 — — 2 7.05
CHEMBL1779337 — — 1 6.96
CHEMBL1779212 — — 2 6.32
CHEMBL1779210 — — 2 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779340 — IC50 = 3.0 nM 8.52
CHEMBL429910 DAPAGLIFLOZIN IC50 = 3.0 nM 8.52
CHEMBL1779217 — IC50 = 3.0 nM 8.52
CHEMBL1779339 — IC50 = 4.0 nM 8.40
CHEMBL1779345 — IC50 = 5.0 nM 8.30
CHEMBL1779338 — IC50 = 5.0 nM 8.30
CHEMBL1779336 — IC50 = 7.0 nM 8.15
CHEMBL1779223 — IC50 = 7.0 nM 8.15
CHEMBL1779343 — IC50 = 8.0 nM 8.10
CHEMBL1779214 — IC50 = 8.0 nM 8.10
CHEMBL1779344 — IC50 = 10.0 nM 8.00
CHEMBL1762505 — IC50 = 10.0 nM 8.00
CHEMBL1779218 — IC50 = 10.0 nM 8.00
CHEMBL1779341 — IC50 = 12.0 nM 7.92
CHEMBL1779219 — IC50 = 12.0 nM 7.92
CHEMBL1779221 — IC50 = 13.0 nM 7.89
CHEMBL1779216 — IC50 = 13.0 nM 7.89
CHEMBL1779220 — IC50 = 14.0 nM 7.85
CHEMBL1779207 — IC50 = 21.0 nM 7.68
CHEMBL1779208 — IC50 = 22.0 nM 7.66
CHEMBL1779215 — IC50 = 23.0 nM 7.64
CHEMBL1779205 — IC50 = 36.0 nM 7.44
CHEMBL1779222 — IC50 = 41.0 nM 7.39
CHEMBL1779203 — IC50 = 57.0 nM 7.24
CHEMBL1779209 — IC50 = 59.0 nM 7.23
CHEMBL1779213 — IC50 = 73.0 nM 7.14
CHEMBL1779211 — IC50 = 89.0 nM 7.05
CHEMBL1779337 — IC50 = 110.0 nM 6.96
CHEMBL1779212 — IC50 = 480.0 nM 6.32
CHEMBL1779210 — IC50 = 660.0 nM 6.18
CHEMBL1779342 — IC50 = 5100.0 nM 5.29
CHEMBL1779206 — IC50 = 9800.0 nM 5.01
CHEMBL1779204 — IC50 = 10000.0 nM 5.00
CHEMBL1779206 — Inhibition = 95.0 % -
CHEMBL1779205 — Inhibition = 100.0 % -
CHEMBL1779204 — Inhibition = 95.0 % -
CHEMBL1779211 — Inhibition = 100.0 % -
CHEMBL1779212 — Inhibition = 100.0 % -
CHEMBL1779213 — Inhibition = 98.0 % -
CHEMBL1779214 — Inhibition = 100.0 % -
CHEMBL1779215 — Inhibition = 100.0 % -
CHEMBL1779208 — Inhibition = 100.0 % -
CHEMBL1779217 — Inhibition = 100.0 % -
CHEMBL1779218 — Inhibition = 100.0 % -
CHEMBL1779219 — Inhibition = 100.0 % -
CHEMBL1779220 — Inhibition = 100.0 % -
CHEMBL1779221 — Inhibition = 100.0 % -
CHEMBL1779216 — Inhibition = 100.0 % -
CHEMBL1779203 — Inhibition = 100.0 % -
CHEMBL1762505 — Inhibition = 100.0 % -