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Assay Detail

CHEMBL650716

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

Functional
In vitro ability to inhibit glucose stimulated insulin release in beta-TC6 cells from rat islets
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Beta-TC6
Confidence 1 — Organism
Curated By Expert

Target

Beta-TC6 (CHEMBL614357)
Type CELL-LINE
Organism Mus musculus

Publication

Arylcyanoguanidines as activators of Kir6.2/SUR1K ATP channels and inhibitors of insulin release.
Tagmose TM, Schou SC, Mogensen JP, Nielsen FE, Arkhammar PO, Wahl P, Hansen BS, Worsaae A, Boonen HC, Antoine MH, Lebrun P, Hansen JB.
J Med Chem (2004) 47 : 3202 -3211
PubMed 15163199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.05 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88083 1 5.92
CHEMBL48923 1 5.70
CHEMBL431255 1 5.55
CHEMBL50179 1 5.38
CHEMBL107548 1 5.36
CHEMBL301508 1 5.30
CHEMBL420858 1 5.28
CHEMBL111335 1 5.26
CHEMBL109180 1 4.86
CHEMBL110501 1 4.79
CHEMBL181 DIAZOXIDE 4.0 1 4.65
CHEMBL324456 1 4.54
CHEMBL110551 1 4.40
CHEMBL109198 1 4.38
CHEMBL298121 1 4.31
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88083 IC50 = 1200.0 nM 5.92
CHEMBL48923 IC50 = 2000.0 nM 5.70
CHEMBL431255 IC50 = 2800.0 nM 5.55
CHEMBL50179 IC50 = 4200.0 nM 5.38
CHEMBL107548 IC50 = 4400.0 nM 5.36
CHEMBL301508 IC50 = 5000.0 nM 5.30
CHEMBL420858 IC50 = 5200.0 nM 5.28
CHEMBL111335 IC50 = 5450.0 nM 5.26
CHEMBL109180 IC50 = 13700.0 nM 4.86
CHEMBL110501 IC50 = 16100.0 nM 4.79
CHEMBL181 DIAZOXIDE IC50 = 22400.0 nM 4.65
CHEMBL324456 IC50 = 28700.0 nM 4.54
CHEMBL110551 IC50 = 39800.0 nM 4.40
CHEMBL109198 IC50 = 41400.0 nM 4.38
CHEMBL298121 IC50 = 48500.0 nM 4.31
CHEMBL1159 PINACIDIL ANHYDROUS IC50 > 100000.0 nM -