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Assay Detail

CHEMBL4480253

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

Binding
Inhibition of SETD8 (unknown origin) using biotin-labeled histone H4 (1 to 24 residues) as substrate incubated for 1 hr in presence of [3H-Me]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

Design, synthesis, and protein methyltransferase activity of a unique set of constrained amine containing compounds.
Zhou H, Che X, Bao G, Wang N, Peng L, Barnash KD, Frye SV, James LI, Bai X.
Bioorg Med Chem Lett (2016) 26 : 4436 -4440
PubMed 27528434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.19 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318284 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318284 IC50 = 6500.0 nM 5.19