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Assay Detail

CHEMBL4307073

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

Binding
Binding affinity to human recombinant PRMT5/MEP50 expressed in baculovirus infected High-five cells using histone 4 peptide as substrate assessed as inhibitory constant in presence of [3H]SAM measured upto 120 mins by jump dilution experiment based assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors.
Lin H, Wang M, Zhang YW, Tong S, Leal RA, Shetty R, Vaddi K, Luengo JI.
ACS Med Chem Lett (2019) 10 : 1033 -1038
PubMed 31312404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.26 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4518534 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4518534 Ki = 55.0 nM 7.26