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Assay Detail

CHEMBL3859787

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

Binding
Inhibition of recombinant MLL1 (unknown origin) interaction with recombinant ASH2L/RBBP5/WDR5 (unknown origin) assessed as decrease in histone methylation after 60 mins by Alpha Screen assay
3
Total Activities
3
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 3 5.55 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3883592 1 6.05
CHEMBL3907289 1 5.34
CHEMBL3957478 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3883592 IC50 = 900.0 nM 6.05
CHEMBL3907289 IC50 = 4600.0 nM 5.34
CHEMBL3957478 IC50 = 5400.0 nM 5.27