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Assay Detail

CHEMBL5318924

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

Binding
Inhibition of N-terminal polyhistidine tagged human recombinant NSD2 SET domain (934 to 1241 residues) expressed in Escherichia coli using SAM as substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by MTase-Glo assay
1
Total Activities
1
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

Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Tang H, Yu A, Xing L, Chen X, Ding H, Yang H, Song Z, Shi Q, Geng M, Huang X, Zhang A.
J Med Chem (2023) 66 : 1634 -1651
PubMed 36642961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.77 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337173 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337173 IC50 = 170.0 nM 6.77