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Assay Detail

CHEMBL5141671

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

Binding
Binding affinity to N-terminal GST-tagged human NSD2 PWWP1 domain (208 to 369 residues) expressed in Escherichia coli BL2I (DE3) cells assessed as dissociation constant by isothermal titration calorimetry 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

Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos.
Meng F, Xu C, Park KS, Kaniskan HÜ, Wang GG, Jin J.
J Med Chem (2022) 65 : 10611 -10625
PubMed 35895319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.10 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5200945 1 6.30
CHEMBL5193618 1 6.05
CHEMBL5195436 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5200945 Kd = 500.0 nM 6.30
CHEMBL5193618 Kd = 900.0 nM 6.05
CHEMBL5195436 Kd = 1100.0 nM 5.96