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Assay Detail

CHEMBL3875503

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

Binding
Binding affinity to human WDR5 by isothermal titration calorimetry
3
Total Activities
3
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

High-affinity small molecular blockers of mixed lineage leukemia 1 (MLL1)-WDR5 interaction inhibit MLL1 complex H3K4 methyltransferase activity.
Li DD, Chen WL, Wang ZH, Xie YY, Xu XL, Jiang ZY, Zhang XJ, You QD, Guo XK.
Eur J Med Chem (2016) 124 : 480 -489
PubMed 27598236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.56 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3884726 1 8.12
CHEMBL3884329 1 7.87
CHEMBL3885241 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3884726 Kd = 7.5 nM 8.12
CHEMBL3884329 Kd = 13.6 nM 7.87
CHEMBL3885241 Kd = 202.0 nM 6.70