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Assay Detail

CHEMBL4832215

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

Binding
Inhibition of MLL1 (unknown origin)-mediated H3K4 methylation using histone H3 and SAM as substrate incubated for 30 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 2A (CHEMBL1293299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.
Chen W, Chen X, Li D, Wang X, Long G, Jiang Z, You Q, Guo X.
Eur J Med Chem (2021) 223 : 113677 -113677
PubMed 34225179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.76 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4861912 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4861912 IC50 = 174.0 nM 6.76