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Assay Detail

CHEMBL5388285

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

Binding
Inhibition of 15N-labeled NSD2 (953 to 1240 residues) (unknown origin) expressed in Escherichia coli BL21 DE3 using H3K36 as substrate incubated for 60 mins by Alphascreen assay
3
Total Activities
3
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

Histone-lysine N-methyltransferase NSD2 (CHEMBL3108645)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent advances in nuclear receptor-binding SET domain 2 (NSD2) inhibitors: An update and perspectives.
Zhang L, Zha X.
Eur J Med Chem (2023) 250 : 115232 -115232
PubMed 36863225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.19 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5441106 1 5.75
CHEMBL3414624 1 5.48
CHEMBL1214186 SINEFUNGIN 2.0 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5441106 IC50 = 1800.0 nM 5.75
CHEMBL3414624 IC50 = 3300.0 nM 5.48
CHEMBL1214186 SINEFUNGIN IC50 = 46000.0 nM 4.34