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Assay Detail

CHEMBL3591656

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

Binding
Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-375
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 6 (CHEMBL1275221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.
Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA.
ACS Med Chem Lett (2015) 6 : 655 -659
PubMed 26101569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.20 6.20
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589039 2 6.20
CHEMBL3589038 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589039 IC50 = 637.0 nM 6.20
CHEMBL3589038 IC50 > 20000.0 nM -
CHEMBL3589039 Inhibition - % -