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Assay Detail

CHEMBL4673852

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

Binding
Inhibition of recombinant SETD8 catalytic domain (unknown origin) (232 to 393 residues) expressed in Escherichia coli assessed as reduction in incorporation of [3H]-labeled methyl group into biotinylated H4 (1 to 24) peptide measured after 5 hrs using [3H-SAM] by scintillation proximity 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

N-lysine methyltransferase KMT5A (CHEMBL1795176)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.
Butler KV,Ma A,Yu W,Li F,Tempel W,Babault N,Pittella-Silva F,Shao J,Wang J,Luo M,Vedadi M,Brown PJ,Arrowsmith CH,Jin J
J Med Chem (2016) 59 : 9881 -9889
PubMed 27804297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.09 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4791952 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4791952 IC50 = 804.0 nM 6.09