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Assay Detail

CHEMBL3784078

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

Binding
Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 6 (CHEMBL1275221)
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 17 4.32 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3780926 1 6.64
CHEMBL3780701 1 5.68
CHEMBL3780444 1 5.30
CHEMBL3763993 1 4.62
CHEMBL3781561 1 4.34
CHEMBL3780738 1 4.16
CHEMBL3779956 1 4.14
CHEMBL3780979 1 4.00
CHEMBL3781201 1 4.00
CHEMBL3402235 1 3.98
CHEMBL3780615 1 3.90
CHEMBL3781682 1 3.87
CHEMBL3781603 1 3.84
CHEMBL3781043 1 3.77
CHEMBL3781266 1 3.44
CHEMBL437 SULFATHIAZOLE 4.0 1 3.37
CHEMBL3781841 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3780926 IC50 = 230.0 nM 6.64
CHEMBL3780701 IC50 = 2100.0 nM 5.68
CHEMBL3780444 IC50 = 5000.0 nM 5.30
CHEMBL3763993 IC50 = 24000.0 nM 4.62
CHEMBL3781561 IC50 = 46000.0 nM 4.34
CHEMBL3780738 IC50 = 69000.0 nM 4.16
CHEMBL3779956 IC50 = 72000.0 nM 4.14
CHEMBL3780979 IC50 = 100000.0 nM 4.00
CHEMBL3781201 IC50 = 99000.0 nM 4.00
CHEMBL3402235 IC50 = 104000.0 nM 3.98
CHEMBL3780615 IC50 = 125000.0 nM 3.90
CHEMBL3781682 IC50 = 136000.0 nM 3.87
CHEMBL3781603 IC50 = 146000.0 nM 3.84
CHEMBL3781043 IC50 = 170000.0 nM 3.77
CHEMBL3781266 IC50 = 360000.0 nM 3.44
CHEMBL437 SULFATHIAZOLE IC50 = 430000.0 nM 3.37
CHEMBL3781841 IC50 > 200000.0 nM -