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Assay Detail

CHEMBL4392562

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

Binding
Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immunohistochemistry method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 5 (CHEMBL1795116)
Type SINGLE PROTEIN
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 14 8.20 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541714 1 9.80
CHEMBL4249337 ONAMETOSTAT 1.0 1 9.60
CHEMBL4543007 1 9.40
CHEMBL4579773 1 8.90
CHEMBL4577464 1 8.70
CHEMBL4539612 1 8.40
CHEMBL4564327 1 8.20
CHEMBL4541070 1 8.20
CHEMBL4439077 1 8.10
CHEMBL4540972 1 7.29
CHEMBL4556400 1 7.10
CHEMBL4576734 1 6.90
CHEMBL4589179 1 5.97
CHEMBL4454890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541714 IC50 = 0.16 nM 9.80
CHEMBL4249337 ONAMETOSTAT IC50 = 0.25 nM 9.60
CHEMBL4543007 IC50 = 0.4 nM 9.40
CHEMBL4579773 IC50 = 1.26 nM 8.90
CHEMBL4577464 IC50 = 2.0 nM 8.70
CHEMBL4539612 IC50 = 3.98 nM 8.40
CHEMBL4564327 IC50 = 6.31 nM 8.20
CHEMBL4541070 IC50 = 6.31 nM 8.20
CHEMBL4439077 IC50 = 7.9 nM 8.10
CHEMBL4540972 IC50 = 51.3 nM 7.29
CHEMBL4556400 IC50 = 79.4 nM 7.10
CHEMBL4576734 IC50 = 125.0 nM 6.90
CHEMBL4589179 IC50 = 1070.0 nM 5.97
CHEMBL4454890 IC50 - -