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Assay Detail

CHEMBL5529508

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

Binding
Antagonist activity at human NOD2 expressed in HEK-Blue cells coexpressing NF-kappaB-inducible SEAP reporter gene assessed as inhibition of MDP-induced NF-kappaB transcriptional activity by measuring decrease in SEAP activity preincubated for 1 hr followed by MDP addition and measured after 18 hrs by spectrophotometric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-Blue hNOD2
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of 2,3-Diaminoindole Derivatives as a Novel Class of NOD Antagonists.
Russo C, Russomanno P, D'Amore VM, Alfano AI, Santoro F, Guzelj S, Gobec M, Amato J, Pagano B, Marinelli L, Carotenuto A, Tron GC, Di Leva FS, Jakopin Ž, Brancaccio D, Giustiniano M.
J Med Chem (2024) 67 : 3004 -3017
PubMed 38301029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.50 4.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566720 1 4.79
CHEMBL5595306 1 4.68
CHEMBL5591686 1 4.38
CHEMBL5594651 1 4.37
CHEMBL1412853 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566720 IC50 = 16100.0 nM 4.79
CHEMBL5595306 IC50 = 20800.0 nM 4.68
CHEMBL5591686 IC50 = 41900.0 nM 4.38
CHEMBL5594651 IC50 = 42600.0 nM 4.37
CHEMBL1412853 IC50 = 54900.0 nM 4.26