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Assay Detail

CHEMBL796592

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

Functional
Relaxation of phenylephrine precontracted rat isolated aorta rings.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

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 20 4.84 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298121 1 6.52
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 6.10
CHEMBL295342 1 6.05
CHEMBL48923 1 5.25
CHEMBL88083 1 4.96
CHEMBL109180 1 4.92
CHEMBL301508 1 4.91
CHEMBL181 DIAZOXIDE 4.0 1 4.89
CHEMBL420858 1 4.75
CHEMBL50179 1 4.73
CHEMBL107548 1 4.69
CHEMBL431255 1 4.55
CHEMBL110551 1 4.52
CHEMBL110501 1 4.36
CHEMBL111332 1 4.28
CHEMBL109198 1 4.21
CHEMBL324456 1 4.12
CHEMBL111048 1 4.12
CHEMBL107725 1 4.07
CHEMBL111335 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298121 IC50 = 300.0 nM 6.52
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 800.0 nM 6.10
CHEMBL295342 IC50 = 900.0 nM 6.05
CHEMBL48923 IC50 = 5600.0 nM 5.25
CHEMBL88083 IC50 = 11000.0 nM 4.96
CHEMBL109180 IC50 = 11900.0 nM 4.92
CHEMBL301508 IC50 = 12400.0 nM 4.91
CHEMBL181 DIAZOXIDE IC50 = 12800.0 nM 4.89
CHEMBL420858 IC50 = 17600.0 nM 4.75
CHEMBL50179 IC50 = 18700.0 nM 4.73
CHEMBL107548 IC50 = 20300.0 nM 4.69
CHEMBL431255 IC50 = 27900.0 nM 4.55
CHEMBL110551 IC50 = 30000.0 nM 4.52
CHEMBL110501 IC50 = 43800.0 nM 4.36
CHEMBL111332 IC50 = 52000.0 nM 4.28
CHEMBL109198 IC50 = 61000.0 nM 4.21
CHEMBL324456 IC50 = 75000.0 nM 4.12
CHEMBL111048 IC50 = 75000.0 nM 4.12
CHEMBL107725 IC50 = 85000.0 nM 4.07
CHEMBL111335 IC50 > 300000.0 nM -