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Assay Detail

CHEMBL3239252

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

Binding
Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 5 (CHEMBL1795116)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
Yan L, Yan C, Qian K, Su H, Kofsky-Wofford SA, Lee WC, Zhao X, Ho MC, Ivanov I, Zheng YG.
J Med Chem (2014) 57 : 2611 -2622
PubMed 24564570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.36 4.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142304 STILBAMIDINE 2.0 1 4.36
CHEMBL24057 FURAMIDINE -1.0 1 -
CHEMBL424121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142304 STILBAMIDINE IC50 = 44100.0 nM 4.36
CHEMBL24057 FURAMIDINE IC50 = 166000.0 nM -
CHEMBL424121 IC50 = 186000.0 nM -