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Assay Detail

CHEMBL4404242

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

Binding
Inhibition of rabbit skeletal muscle microsomes SERCA1a incubated for 10 mins by enzyme-coupled method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 (CHEMBL4693)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective.
Peterková L, Kmoníčková E, Ruml T, Rimpelová S.
J Med Chem (2020) 63 : 1937 -1963
PubMed 32030976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.21 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1208858 CALMIDAZOLIUM CHLORIDE 1 6.30
CHEMBL13045 CHELERYTHRINE 1 5.92
CHEMBL726 FLUPHENAZINE 4.0 1 4.82
CHEMBL71 CHLORPROMAZINE 4.0 1 4.64
CHEMBL422 TRIFLUOPERAZINE 4.0 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1208858 CALMIDAZOLIUM CHLORIDE IC50 = 500.0 nM 6.30
CHEMBL13045 CHELERYTHRINE IC50 = 1200.0 nM 5.92
CHEMBL726 FLUPHENAZINE IC50 = 15000.0 nM 4.82
CHEMBL71 CHLORPROMAZINE IC50 = 23000.0 nM 4.64
CHEMBL422 TRIFLUOPERAZINE IC50 = 45000.0 nM 4.35