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Assay Detail

CHEMBL3859795

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

Binding
Inhibition of His-SUMO-fused MLL1 (3762 to 3969 residues) interaction with His-SUMO-fused ASH2L/RBBP5/WDR5 (23 to 334 residues) (unknown origin) expressed in Escherichia coli BL21 DE3 pLyss codon (+) assessed as decrease in methylation of Lys4 residue of histone H3 10-residue peptide using [3H]-S-adenosylmethionine as methyl donor after 2 hrs by scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

MLL1/ASH2L/RBBP5/WDR5 complex (CHEMBL3137282)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction.
Li DD, Wang ZH, Chen WL, Xie YY, You QD, Guo XK.
Bioorg Med Chem (2016) 24 : 6109 -6118
PubMed 27720555 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.52 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3798088 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3798088 IC50 = 300.0 nM 6.52