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Assay Detail

CHEMBL3859786

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

Binding
Inhibition of C-terminal 5-FAM-ARTEVHLRKS binding to WDR5 (unknown origin) by fluorescence polarization assay
22
Total Activities
22
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

WD repeat-containing protein 5 (CHEMBL1075317)
Type SINGLE PROTEIN
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 22 6.64 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3957478 1 7.58
CHEMBL3907289 1 7.33
CHEMBL3962459 1 7.23
CHEMBL3913104 1 6.79
CHEMBL3971604 1 6.61
CHEMBL3903051 1 6.58
CHEMBL3922104 1 6.55
CHEMBL3942025 1 6.36
CHEMBL3950744 1 6.34
CHEMBL3904098 1 6.32
CHEMBL3982971 1 6.09
CHEMBL3894097 1 5.93
CHEMBL3953704 1 -
CHEMBL3906985 1 -
CHEMBL3893446 1 -
CHEMBL3965924 1 -
CHEMBL3936042 1 -
CHEMBL3956505 1 -
CHEMBL3929919 1 -
CHEMBL3943757 1 -
CHEMBL3935228 1 -
CHEMBL3938878 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3957478 IC50 = 26.4 nM 7.58
CHEMBL3907289 IC50 = 46.5 nM 7.33
CHEMBL3962459 IC50 = 58.8 nM 7.23
CHEMBL3913104 IC50 = 162.4 nM 6.79
CHEMBL3971604 IC50 = 244.9 nM 6.61
CHEMBL3903051 IC50 = 263.5 nM 6.58
CHEMBL3922104 IC50 = 283.9 nM 6.55
CHEMBL3942025 IC50 = 433.2 nM 6.36
CHEMBL3950744 IC50 = 454.0 nM 6.34
CHEMBL3904098 IC50 = 483.5 nM 6.32
CHEMBL3982971 IC50 = 811.6 nM 6.09
CHEMBL3894097 IC50 = 1171.0 nM 5.93
CHEMBL3953704 IC50 > 20.0 nM -
CHEMBL3906985 IC50 > 20.0 nM -
CHEMBL3893446 IC50 > 20.0 nM -
CHEMBL3965924 IC50 > 20.0 nM -
CHEMBL3936042 IC50 > 20.0 nM -
CHEMBL3956505 IC50 > 20.0 nM -
CHEMBL3929919 IC50 > 20.0 nM -
CHEMBL3943757 IC50 > 20.0 nM -
CHEMBL3935228 IC50 > 20.0 nM -
CHEMBL3938878 IC50 > 20.0 nM -