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Assay Detail

CHEMBL4411980

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

ADMET
Negative inotropic activity in guinea pig spontaneously beating spontaneously beating right atrium assessed as decrease in developed tension
8
Total Activities
8
Compounds Tested
1
Activity Types
0
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

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 8 5.85 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4590632 1 6.33
CHEMBL4449273 1 6.29
CHEMBL514508 1 5.97
CHEMBL4573134 1 5.73
CHEMBL4577064 1 5.66
CHEMBL4574696 1 5.66
CHEMBL475745 1 5.61
CHEMBL4549511 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4590632 EC50 = 470.0 nM 6.33
CHEMBL4449273 EC50 = 510.0 nM 6.29
CHEMBL514508 EC50 = 1080.0 nM 5.97
CHEMBL4573134 EC50 = 1870.0 nM 5.73
CHEMBL4577064 EC50 = 2180.0 nM 5.66
CHEMBL4574696 EC50 = 2200.0 nM 5.66
CHEMBL475745 EC50 = 2480.0 nM 5.61
CHEMBL4549511 EC50 = 2870.0 nM 5.54