Assay Detail

CHEMBL5345898

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

Binding

Inhibition of human recombinant IKKepsilon by microfluidic mobility shift assay

ChEMBL ↗

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Target

Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗

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Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Inhibitor of nuclear factor kappa-B kinase subunit epsilon

CHEMBL3529

Anchored from Assay target.

Protein identity Inhibitor of nuclear factor kappa-B kinase subunit epsilon

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.

Temal-Laib T, Peixoto C, Desroy N, De Lemos E, Bonnaterre F, Bienvenu N, Picolet O, Sartori E, Bucher D, López-Ramos M, Roca Magadán C, Laenen W, Flower T, Mollat P, Bugaud O, Touitou R, Pereira Fernandes A, Lavazais S, Monjardet A, Borgonovi M, Gosmini R, Brys R, Amantini D, De Vos S, Andrews M.
J Med Chem (2024) 67 : 380 -401
PubMed 38147525 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.16	7.16

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5407103	—	—	1	7.16

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5407103	—	IC50	=	70.0	nM	7.16