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Assay Detail

CHEMBL3801644

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

Binding
Inhibition of SUMO-His-tagged MLL1 activity (unknown origin) expressed in Escherichia coli BL21(DE3) pLysS cells using histone H3 as substrate by scintillation counting method in presence of [3H]SAM
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

Histone-lysine N-methyltransferase 2A (CHEMBL1293299)
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 6.50 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3798088 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3798088 IC50 = 320.0 nM 6.50