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Assay Detail

CHEMBL4133043

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

Functional
Vasorelaxant activity in Sprague-Dawley rat endothelium denuded mesentric artery rings assessed as inhibition of phenylephrine-induced contraction
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Mesenteric artery
Confidence 1 — Organism
Curated By Intermediate

Target

Mesenteric artery (CHEMBL4296533)
Type TISSUE
Organism Rattus norvegicus

Publication

Novel rhynchophylline analogues as microvascular relaxation agents for the treatment of microvascular dysfunction caused by diabetes.
Guo W, Zhu H, Wang Z, Chen JA, Wu J, Zhu Y, Gu X.
Eur J Med Chem (2017) 139 : 657 -664
PubMed 28846966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.17 5.92
Emax 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168427 2 5.92
CHEMBL4172138 2 5.29
CHEMBL4164257 2 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168427 IC50 = 1200.0 nM 5.92
CHEMBL4172138 IC50 = 5150.0 nM 5.29
CHEMBL4164257 IC50 = 49890.0 nM 4.30
CHEMBL4168427 Emax = 99.74 % -
CHEMBL4172138 Emax = 100.76 % -
CHEMBL4164257 Emax = 86.29 % -