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Assay Detail

CHEMBL4307075

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Functional
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Granta-519
Confidence 1 — Organism
Curated By Autocuration

Target

Granta-519 (CHEMBL4483240)
Type CELL-LINE
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 6.99 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4539373 1 7.32
CHEMBL4518534 1 7.22
CHEMBL4548376 1 6.85
CHEMBL4451469 1 6.57
CHEMBL4475046 1 -
CHEMBL4585395 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4539373 IC50 = 48.0 nM 7.32
CHEMBL4518534 IC50 = 60.0 nM 7.22
CHEMBL4548376 IC50 = 140.0 nM 6.85
CHEMBL4451469 IC50 = 270.0 nM 6.57
CHEMBL4475046 IC50 > 1000.0 nM -
CHEMBL4585395 IC50 > 1000.0 nM -