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Assay Detail

CHEMBL5523023

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

Binding
Inhibition of NIK (unknown origin) expressed in COS-7 cells co-expressing NF-KappaB luciferase reporter assessed as suppression of luciferase reporter measured after 24 by beta-Gal activity assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis Treatment.
Zhang N, Shen S, Yang M, He S, Liu C, Li H, Lu T, Liu H, Hu Q, Tang W, Chen Y.
J Med Chem (2024) 67 : 5617 -5641
PubMed 38563549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.76 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187788 1 6.04
CHEMBL5562073 1 5.92
CHEMBL5542106 1 5.88
CHEMBL5556543 1 5.85
CHEMBL5567931 1 5.82
CHEMBL5564890 1 5.66
CHEMBL5542501 1 5.65
CHEMBL5542810 1 5.61
CHEMBL5523606 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187788 IC50 = 910.0 nM 6.04
CHEMBL5562073 IC50 = 1190.0 nM 5.92
CHEMBL5542106 IC50 = 1330.0 nM 5.88
CHEMBL5556543 IC50 = 1410.0 nM 5.85
CHEMBL5567931 IC50 = 1510.0 nM 5.82
CHEMBL5564890 IC50 = 2170.0 nM 5.66
CHEMBL5542501 IC50 = 2230.0 nM 5.65
CHEMBL5542810 IC50 = 2430.0 nM 5.61
CHEMBL5523606 IC50 = 3560.0 nM 5.45