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Assay Detail

CHEMBL4717675

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

ADMET
Inhibition of calcium-induced contraction in K+-depolarized guinea pig longitudinal smooth muscle
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Cavia porcellus
Tissue Ileum
Confidence 1 — Organism
Curated By Autocuration

Target

Ileum (CHEMBL613680)
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
IC50 5 5.01 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764860 1 5.44
CHEMBL1200606 MEXILETINE HYDROCHLORIDE 4.0 1 5.07
CHEMBL4741603 1 4.97
CHEMBL4742143 1 4.86
CHEMBL4746834 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764860 IC50 = 3600.0 nM 5.44
CHEMBL1200606 MEXILETINE HYDROCHLORIDE IC50 = 8500.0 nM 5.07
CHEMBL4741603 IC50 = 10700.0 nM 4.97
CHEMBL4742143 IC50 = 13800.0 nM 4.86
CHEMBL4746834 IC50 = 19600.0 nM 4.71