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Assay Detail

CHEMBL4392552

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

Binding
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histone H4 peptide H-SGRGKGGKGLGKGGAKRHRKVLRDK-Biotin measured after 2 hrs by liquid scintillation counting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

PRMT5/MEP50 complex (CHEMBL3137261)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Nucleoside protein arginine methyltransferase 5 (PRMT5) inhibitors.
Lin H, Luengo JI.
Bioorg Med Chem Lett (2019) 29 : 1264 -1269
PubMed 30956011 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.20 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4585781 1 8.37
CHEMBL4168754 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4585781 IC50 = 4.3 nM 8.37
CHEMBL4168754 IC50 = 9.5 nM 8.02