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Assay Detail

CHEMBL5236414

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Binding
Binding affinity to human PCSK9
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proprotein convertase subtilisin/kexin type 9 (CHEMBL2929)
Type SINGLE PROTEIN
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
Kd 8 7.32 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5271747 1 9.52
CHEMBL5280306 1 8.26
CHEMBL5278292 1 8.21
CHEMBL5273270 1 7.82
CHEMBL5278470 1 6.41
CHEMBL4226740 1 6.16
CHEMBL4227325 1 6.16
CHEMBL5279432 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5271747 Kd = 0.3 nM 9.52
CHEMBL5280306 Kd = 5.5 nM 8.26
CHEMBL5278292 Kd = 6.1 nM 8.21
CHEMBL5273270 Kd = 15.0 nM 7.82
CHEMBL5278470 Kd = 390.0 nM 6.41
CHEMBL4226740 Kd = 700.0 nM 6.16
CHEMBL4227325 Kd = 700.0 nM 6.16
CHEMBL5279432 Kd = 1000.0 nM 6.00