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Assay Detail

CHEMBL5236437

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

Binding
Inhibition of PCSK9-LDLR protein-protein interaction in human HepG2 cells assessed as increase in LDL uptake
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

PCSK9/LDLR (CHEMBL4523996)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Recent Update on the Development of PCSK9 Inhibitors for Hypercholesterolemia Treatment.
Ahamad S, Bhat SA.
J Med Chem (2022) 65 : 15513 -15539
PubMed 36446632 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.32 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5271747 1 6.97
CHEMBL5278292 1 6.77
CHEMBL4228379 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5271747 EC50 = 106.0 nM 6.97
CHEMBL5278292 EC50 = 170.0 nM 6.77
CHEMBL4228379 EC50 = 6000.0 nM 5.22