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Assay Detail

CHEMBL830078

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

Binding
Displacement of [3H]glibenclamide from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

ATP-binding cassette sub-family C member 8 (CHEMBL2071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
Wängler B, Beck C, Shiue CY, Schneider S, Schwanstecher C, Schwanstecher M, Feilen PJ, Alavi A, Rösch F, Schirrmacher R.
Bioorg Med Chem Lett (2004) 14 : 5205 -5209
PubMed 15380228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.08 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1272 REPAGLINIDE 4.0 1 7.30
CHEMBL360610 1 7.08
CHEMBL186684 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1272 REPAGLINIDE Kd = 50.0 nM 7.30
CHEMBL360610 Kd = 83.0 nM 7.08
CHEMBL186684 Kd = 134.0 nM 6.87