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Assay Detail

CHEMBL864943

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

Binding
Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells in presence of 2 mM ATP
3
Total Activities
3
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

New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
Nielsen FE, Ebdrup S, Jensen AF, Ynddal L, Bodvarsdottir TB, Stidsen C, Worsaae A, Boonen HC, Arkhammar PO, Fremming T, Wahl P, Kornø HT, Hansen JB.
J Med Chem (2006) 49 : 4127 -4139
PubMed 16821773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.82 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212041 1 7.09
CHEMBL135191 TIFENAZOXIDE 2.0 1 6.54
CHEMBL181 DIAZOXIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212041 IC50 = 81.0 nM 7.09
CHEMBL135191 TIFENAZOXIDE IC50 = 286.0 nM 6.54
CHEMBL181 DIAZOXIDE IC50 = 194000.0 nM -