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Assay Detail

CHEMBL3824754

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Functional
Vasoprotective activity against oxidative stress-induced impairment of ACh-stimulated vasorelaxation in Sprague-Dawley rat endothelium-intact aortic rings assessed as reduction in L-phenylephrine hydrochloride-induced contraction preincubated for 10 to 20 mins in presence of xanthine-xanthine oxidase system prior to L-phenylephrine hydrochloride addition
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

Publication

On the vasoprotective mechanisms underlying novel β-phosphorylated nitrones: Focus on free radical characterization, scavenging and NO-donation in a biological model of oxidative stress.
Cassien M, Petrocchi C, Thétiot-Laurent S, Robin M, Ricquebourg E, Kandouli C, Asteian A, Rockenbauer A, Mercier A, Culcasi M, Pietri S.
Eur J Med Chem (2016) 119 : 197 -217
PubMed 27162124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.16 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3823412 1 7.55
CHEMBL3823573 1 7.39
CHEMBL3823574 1 7.27
CHEMBL3823604 1 7.17
CHEMBL3824345 1 6.83
CHEMBL13210 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3823412 EC50 = 28.18 nM 7.55
CHEMBL3823573 EC50 = 40.74 nM 7.39
CHEMBL3823574 EC50 = 53.7 nM 7.27
CHEMBL3823604 EC50 = 67.61 nM 7.17
CHEMBL3824345 EC50 = 147.91 nM 6.83
CHEMBL13210 EC50 = 173.78 nM 6.76