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Assay Detail

CHEMBL4736944

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

Binding
Displacement of Halo-tagged Histone H3.3 from Nanoluc-tagged NSD2- PWWP1 (unknown origin) transfected in human U2OS cells preincubated for one day followed by Nano-GloR substrate addition at the next day and measured withing 10 mins by NanoBRET assay
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
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 Small-Molecule Antagonists of the PWWP Domain of NSD2.
Ferreira de Freitas R,Liu Y,Szewczyk MM,Mehta N,Li F,McLeod D,Zepeda-Velázquez C,Dilworth D,Hanley RP,Gibson E,Brown PJ,Al-Awar R,James LI,Arrowsmith CH,Barsyte-Lovejoy D,Min J,Vedadi M,Schapira M,Allali-Hassani A
J Med Chem (2021) 64 : 1584 -1592
PubMed 33522809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 1 - -
IC50 1 4.76 4.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4758943 2 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4758943 IC50 = 17300.0 nM 4.76
CHEMBL4758943 Activity - -