Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4376147

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

Binding
Inhibition of V5-tagged SMYD2 (unknown origin) transfected in human MDA-MB-231 cells co-transfected with FLAG-tagged p53 assessed as reduction in p53 methylation at K370 residue measured after 20 hrs by immunoblot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

N-lysine methyltransferase SMYD2 (CHEMBL2169716)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Taylor AP, Swewczyk M, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, Ferreira de Freitas R, Tatlock J, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown PJ, Arrowsmith CH, Owen DR.
J Med Chem (2019) 62 : 7669 -7683
PubMed 31415173 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.89 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4520134 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4520134 IC50 = 1300.0 nM 5.89