Assay Detail

CHEMBL4717670

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ADMET

Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate

ChEMBL ↗

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Target

Right atrium (CHEMBL2367363) ↗

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Primary target Right atrium

CHEMBL2367363

Anchored from Assay target.

Protein identity Right atrium

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	ADMET
Organism	Cavia porcellus
Tissue	Right cardiac atrium
Confidence	1 — Organism
Curated By	Autocuration

Target

Right atrium (CHEMBL2367363) ↗

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	2	6.37	7.85

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1200606	MEXILETINE HYDROCHLORIDE	4.0	1	7.85
CHEMBL4746834	—	—	1	4.88

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1200606	MEXILETINE HYDROCHLORIDE	EC50	=	14.0	nM	7.85
CHEMBL4746834	—	EC50	=	13100.0	nM	4.88