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Assay Detail

CHEMBL5318921

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

Binding
Inhibition of human MMSET (973 to 1203 residues) expressed in Escherichia coli BL21 (DE3) using S-adenosyl-methionine as substrate incubated for 60 mins by AlphaScreen 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 5.48 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414624 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414624 IC50 = 3300.0 nM 5.48