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Assay Detail

CHEMBL4138641

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

Binding
Inhibition of PRMT1 (unknown origin) assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histone H4 peptide H4-20-Biotin at 10 uM pre-incubated for 3 mins before [3H]-SAM addition and measured after 15 mins by scintillation proximity assay
5
Total Activities
5
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

Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
Zhang J, Qian K, Yan C, He M, Jassim BA, Ivanov I, Zheng YG.
Medchemcomm (2017) 8 : 440 -444
PubMed 28649316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.44 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3245413 1 4.89
CHEMBL24057 FURAMIDINE -1.0 1 4.66
CHEMBL25105 HEXAMIDINE 2.0 1 4.28
CHEMBL142304 STILBAMIDINE 2.0 1 4.28
CHEMBL55 PENTAMIDINE 4.0 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3245413 IC50 = 13000.0 nM 4.89
CHEMBL24057 FURAMIDINE IC50 = 22000.0 nM 4.66
CHEMBL25105 HEXAMIDINE IC50 = 52000.0 nM 4.28
CHEMBL142304 STILBAMIDINE IC50 = 52000.0 nM 4.28
CHEMBL55 PENTAMIDINE IC50 = 81000.0 nM 4.09