Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2209109

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

Binding
Inhibition of PRMT3 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 3 (CHEMBL5891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH.
ACS Med Chem Lett (2012) 3 : 1091 -1096
PubMed 24900432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.20 4.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204997 1 4.27
CHEMBL2204995 1 4.13
CHEMBL2204998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204997 IC50 = 54000.0 nM 4.27
CHEMBL2204995 IC50 = 74000.0 nM 4.13
CHEMBL2204998 IC50 > 100000.0 nM -