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Assay Detail

CHEMBL4404229

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

Binding
Inhibition of human SERCA2b expressed in COS7 cells microsomal membranes preincubated for 10 mins followed by addition of ATP and measured after 40 mins by ELISA method
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (CHEMBL3901)
Type SINGLE PROTEIN
Organism Homo sapiens

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 3 6.48 7.05
Ki 1 4.28 4.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468766 1 7.05
CHEMBL4534285 1 6.68
CHEMBL480626 1 5.70
CHEMBL140 CURCUMIN 3.0 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468766 IC50 = 90.0 nM 7.05
CHEMBL4534285 IC50 = 210.0 nM 6.68
CHEMBL480626 IC50 = 2000.0 nM 5.70
CHEMBL140 CURCUMIN Ki = 53000.0 nM 4.28