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Assay Detail

CHEMBL1038191

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Sulfonylurea receptor 1, Kir6.2 (CHEMBL2096972)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity.
Pirotte B, de Tullio P, Nguyen QA, Somers F, Fraikin P, Florence X, Wahl P, Hansen JB, Lebrun P.
J Med Chem (2010) 53 : 147 -154
PubMed 19919106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.87 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL568795 1 7.10
CHEMBL181 DIAZOXIDE 4.0 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL568795 EC50 = 80.0 nM 7.10
CHEMBL181 DIAZOXIDE EC50 = 23500.0 nM 4.63