Assay Detail

CHEMBL1771943

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Binding

Inhibition of rat SGLT2

ChEMBL ↗

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Target

Sodium/glucose cotransporter 2 (CHEMBL4316) ↗

Open DB target context

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Sodium/glucose cotransporter 2 (CHEMBL4316) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium/glucose cotransporter 2

CHEMBL4316

Anchored from Assay target.

Protein identity Sodium/glucose cotransporter 2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Rattus norvegicus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sodium/glucose cotransporter 2 (CHEMBL4316) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.

Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T.
J Med Chem (2011) 54 : 2952 -2960
PubMed 21449606 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.94	8.94

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1770248	ERTUGLIFLOZIN	4.0	1	8.94

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1770248	ERTUGLIFLOZIN	IC50	=	1.15	nM	8.94