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Assay Detail

CHEMBL3224281

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Functional
Vasorelaxant activity in Sprague-Dawley rat thoracic aorta with intact endothelium assessed as inhibition of Ca2+-induced contraction after 20 mins
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Thoracic aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Thoracic aorta (CHEMBL2367449)
Type TISSUE
Organism Rattus norvegicus

Publication

Water soluble flavonol prodrugs that protect against ischaemia-reperfusion injury in rat hindlimb and sheep heart
Williams SJ, Thomas CJ, Boujaoude M, Gannon CT, Zanatta SD, Jarrott B, May CN, Woodman OL
Medchemcomm (2011) 2 : 321 -324
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.11 5.37
Rmax 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294009 FLAVONOL 2 5.37
CHEMBL122701 2 5.02
CHEMBL272682 2 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294009 FLAVONOL IC50 = 4265.8 nM 5.37
CHEMBL122701 IC50 = 9549.93 nM 5.02
CHEMBL272682 IC50 = 11748.98 nM 4.93
CHEMBL294009 FLAVONOL Rmax = 19.0 % -
CHEMBL272682 Rmax = 70.0 % -
CHEMBL122701 Rmax = 89.0 % -