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Assay Detail

CHEMBL4411985

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

ADMET
Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Left atrium (CHEMBL2367407)
Type TISSUE
Organism Cavia porcellus

Publication

Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment.
Bisi A, Arribas RL, Micucci M, Budriesi R, Feoli A, Castellano S, Belluti F, Gobbi S, de Los Rios C, Rampa A.
Eur J Med Chem (2019) 163 : 394 -402
PubMed 30530190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.10 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4590632 1 6.66
CHEMBL193 NIFEDIPINE 4.0 1 6.58
CHEMBL4558734 1 6.50
CHEMBL475745 1 6.37
CHEMBL4549511 1 6.07
CHEMBL514508 1 6.06
CHEMBL4574696 1 5.83
CHEMBL4449273 1 5.72
CHEMBL4573134 1 5.72
CHEMBL4577064 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4590632 EC50 = 220.0 nM 6.66
CHEMBL193 NIFEDIPINE EC50 = 260.0 nM 6.58
CHEMBL4558734 EC50 = 320.0 nM 6.50
CHEMBL475745 EC50 = 430.0 nM 6.37
CHEMBL4549511 EC50 = 850.0 nM 6.07
CHEMBL514508 EC50 = 870.0 nM 6.06
CHEMBL4574696 EC50 = 1490.0 nM 5.83
CHEMBL4449273 EC50 = 1910.0 nM 5.72
CHEMBL4573134 EC50 = 1910.0 nM 5.72
CHEMBL4577064 EC50 = 3650.0 nM 5.44