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Assay Detail

CHEMBL974294

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Binding
Inhibition of human SGLT1 expressed in xenopus laevis oocyte assessed as inhibition of methyl-alpha-D-[14C]glucopyranoside uptake after 1 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium/glucose cotransporter 1 (CHEMBL4979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity.
Vernaleken A, Veyhl M, Gorboulev V, Kottra G, Palm D, Burckhardt BC, Burckhardt G, Pipkorn R, Beier N, van Amsterdam C, Koepsell H.
J Biol Chem (2007) 282 : 28501 -28513
PubMed 17686765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.24 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485830 1 9.80
CHEMBL521026 1 9.77
CHEMBL486028 1 8.70
CHEMBL485831 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485830 IC50 = 0.16 nM 9.80
CHEMBL521026 IC50 = 0.17 nM 9.77
CHEMBL486028 IC50 = 2.0 nM 8.70
CHEMBL485831 IC50 = 2.1 nM 8.68