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Assay Detail

CHEMBL3239251

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

Binding
Inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) 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
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 1 (CHEMBL5524)
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 5.00 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424121 1 5.14
CHEMBL24057 FURAMIDINE -1.0 1 5.03
CHEMBL142304 STILBAMIDINE 2.0 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424121 IC50 = 7200.0 nM 5.14
CHEMBL24057 FURAMIDINE IC50 = 9400.0 nM 5.03
CHEMBL142304 STILBAMIDINE IC50 = 15200.0 nM 4.82