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Assay Detail

CHEMBL5236424

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Binding
Inhibition of PCSK9-LDLR (unknown origin) protein-protein interaction
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 9 5.86 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5278292 1 8.70
CHEMBL5278854 1 6.16
CHEMBL4226740 1 6.10
CHEMBL5287357 1 5.80
CHEMBL5277547 1 5.77
CHEMBL4228379 1 4.95
CHEMBL5285300 1 4.84
CHEMBL5094892 1 4.57
CHEMBL4472590 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5278292 IC50 = 2.0 nM 8.70
CHEMBL5278854 IC50 = 700.0 nM 6.16
CHEMBL4226740 IC50 = 800.0 nM 6.10
CHEMBL5287357 IC50 = 1600.0 nM 5.80
CHEMBL5277547 IC50 = 1700.0 nM 5.77
CHEMBL4228379 IC50 = 11200.0 nM 4.95
CHEMBL5285300 IC50 = 14500.0 nM 4.84
CHEMBL5094892 IC50 = 27120.0 nM 4.57
CHEMBL4472590 IC50 = 285600.0 nM -