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Assay Detail

CHEMBL5364874

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

Binding
Antagonist activity against recombinant human GST-tagged NSD3 PWWP1 domain (247 to 398 residues) expressed in Escherichia coli BL21(DE3) incubated for 60 mins by TR-FRET assay
2
Total Activities
2
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 NSD3 (CHEMBL3108646)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).
Ma Z, Bolinger AA, Chen H, Zhou J.
J Med Chem (2023) 66 : 10991 -11026
PubMed 37578463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.83 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186268 1 6.96
CHEMBL4778517 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186268 IC50 = 110.0 nM 6.96
CHEMBL4778517 IC50 = 200.0 nM 6.70