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Assay Detail

CHEMBL3801643

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

Binding
Inhibition of N-terminal His-tagged WDR5 (24 to 334 residues) (unknown origin) interaction with MLL1 assessed as displacement of 5-Lys-FAM peptide substrate from WDR5 expressed in Escherichia coli Rosetta2(DE3) pLysS cells by fluorescence polarization 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

WD repeat-containing protein 5 (CHEMBL1075317)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R.
J Med Chem (2016) 59 : 2478 -2496
PubMed 26958703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.54 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3799591 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3799591 IC50 = 2.9 nM 8.54