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Assay Detail

CHEMBL3784104

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

Binding
Inhibition of human PRMT1 using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
4
Total Activities
4
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 a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.
Ferreira de Freitas R, Eram MS, Szewczyk MM, Steuber H, Smil D, Wu H, Li F, Senisterra G, Dong A, Brown PJ, Hitchcock M, Moosmayer D, Stegmann CM, Egner U, Arrowsmith C, Barsyte-Lovejoy D, Vedadi M, Schapira M.
J Med Chem (2016) 59 : 1176 -1183
PubMed 26824386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.55 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3780926 1 4.92
CHEMBL3780444 1 4.41
CHEMBL3780701 1 4.32
CHEMBL3781841 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3780926 IC50 = 12000.0 nM 4.92
CHEMBL3780444 IC50 = 39000.0 nM 4.41
CHEMBL3780701 IC50 = 48000.0 nM 4.32
CHEMBL3781841 IC50 > 1000000.0 nM -