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Assay Detail

CHEMBL5333043

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

Binding
Inhibition of SETD8 (unknown origin)
3
Total Activities
3
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

Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Zhao Y, Jiang B, Gu Z, Chen T, Yu W, Liu S, Liu X, Chen D, Li F, Chen W.
Eur J Med Chem (2023) 246 : 115028 -115028
PubMed 36528996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.38 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337173 1 6.68
CHEMBL3414625 1 6.30
CHEMBL580421 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337173 IC50 = 210.0 nM 6.68
CHEMBL3414625 IC50 = 500.0 nM 6.30
CHEMBL580421 IC50 = 700.0 nM 6.16