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Assay Detail

CHEMBL5338633

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

Binding
Inhibition of full-length IRAK4 (unknown origin) in presence of ATP by DELFIA assay
14
Total Activities
14
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

Interleukin-1 receptor-associated kinase 4 (CHEMBL3778)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Wright SW, Farley KA, Han S, Knafels JD, Lee KL.
ACS Med Chem Lett (2024) 15 : 540 -545
PubMed 38628800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.43 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066705 1 10.00
CHEMBL4081711 ZIMLOVISERTIB 2.0 1 9.70
CHEMBL4093120 1 9.52
CHEMBL4091434 1 9.30
CHEMBL4085199 1 9.22
CHEMBL4071526 1 8.72
CHEMBL4084228 1 8.62
CHEMBL4070515 1 8.57
CHEMBL4061801 1 8.43
CHEMBL4092338 1 8.34
CHEMBL4100091 1 8.12
CHEMBL4073250 1 7.62
CHEMBL4076912 1 7.54
CHEMBL4093989 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066705 IC50 = 0.1 nM 10.00
CHEMBL4081711 ZIMLOVISERTIB IC50 = 0.2 nM 9.70
CHEMBL4093120 IC50 = 0.3 nM 9.52
CHEMBL4091434 IC50 = 0.5 nM 9.30
CHEMBL4085199 IC50 = 0.6 nM 9.22
CHEMBL4071526 IC50 = 1.9 nM 8.72
CHEMBL4084228 IC50 = 2.4 nM 8.62
CHEMBL4070515 IC50 = 2.7 nM 8.57
CHEMBL4061801 IC50 = 3.7 nM 8.43
CHEMBL4092338 IC50 = 4.6 nM 8.34
CHEMBL4100091 IC50 = 7.6 nM 8.12
CHEMBL4073250 IC50 = 23.9 nM 7.62
CHEMBL4076912 IC50 = 29.2 nM 7.54
CHEMBL4093989 IC50 = 55000.0 nM 4.26