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Assay Detail

CHEMBL4361890

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

Binding
Protac activity at VHL/IRAK4 in human PBMC assessed as reduction in R848-stimulated IL-8 level preincubated for 18 hrs followed by R848 stimulation and measured after 8 hrs by MSD assay
2
Total Activities
2
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

von Hippel-Lindau disease tumor suppressor/IRAK4 (CHEMBL4523742)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Targeting IRAK4 for Degradation with PROTACs.
Nunes J, McGonagle GA, Eden J, Kiritharan G, Touzet M, Lewell X, Emery J, Eidam H, Harling JD, Anderson NA.
ACS Med Chem Lett (2019) 10 : 1081 -1085
PubMed 31312412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.30 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081711 ZIMLOVISERTIB 2.0 1 7.50
CHEMBL4521789 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081711 ZIMLOVISERTIB IC50 = 31.62 nM 7.50
CHEMBL4521789 IC50 = 79.43 nM 7.10