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Assay Detail

CHEMBL4307074

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Binding
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Granta-519
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 5 (CHEMBL1795116)
Type SINGLE PROTEIN
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
IC50 6 7.44 7.92
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4518534 2 7.92
CHEMBL4539373 1 7.66
CHEMBL4548376 1 7.37
CHEMBL4451469 1 6.80
CHEMBL4475046 1 -
CHEMBL4585395 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4518534 IC50 = 12.0 nM 7.92
CHEMBL4539373 IC50 = 22.0 nM 7.66
CHEMBL4548376 IC50 = 43.0 nM 7.37
CHEMBL4451469 IC50 = 158.0 nM 6.80
CHEMBL4475046 IC50 > 1000.0 nM -
CHEMBL4585395 IC50 > 1000.0 nM -
CHEMBL4518534 Inhibition - % -