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Assay Detail

CHEMBL4717658

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Functional
Antiarrhythmic activity in 50 Hz sinusoidal alternating current-induced guinea pig left atrium arrhythmias model assessed as increase in threshold of ac-arrhythmia measured for every 30 mins relative to control
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Left cardiac atrium
Confidence 1 — Organism
Curated By Autocuration

Target

Left atrium (CHEMBL2367407)
Type TISSUE
Organism Cavia porcellus

Publication

Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues.
Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G
Eur J Med Chem (2016) 121 : 300 -307
PubMed 27267000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.42 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4742143 1 6.37
CHEMBL4741603 1 5.68
CHEMBL4764860 1 5.36
CHEMBL1200606 MEXILETINE HYDROCHLORIDE 4.0 1 4.94
CHEMBL4746834 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4742143 EC50 = 430.0 nM 6.37
CHEMBL4741603 EC50 = 2110.0 nM 5.68
CHEMBL4764860 EC50 = 4360.0 nM 5.36
CHEMBL1200606 MEXILETINE HYDROCHLORIDE EC50 = 11600.0 nM 4.94
CHEMBL4746834 EC50 = 18400.0 nM 4.74