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Assay Detail

CHEMBL4680701

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

Binding
Inhibition of PRMT5 in human Z138 cells assessed as reduction in symmetrical dimethylation of arginine containing substrate using SmD3 as substrate incubated for 4 days by In-cell western assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Z138
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 5 (CHEMBL1795116)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.
Duncan KW,Rioux N,Boriack-Sjodin PA,Munchhof MJ,Reiter LA,Majer CR,Jin L,Johnston LD,Chan-Penebre E,Kuplast KG,Porter Scott M,Pollock RM,Waters NJ,Smith JJ,Moyer MP,Copeland RA,Chesworth R
ACS Med Chem Lett (2016) 7 : 162 -166
PubMed 26985292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.33 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4542380 1 8.52
CHEMBL4060831 1 8.05
CHEMBL3938760 1 7.89
CHEMBL3958947 1 7.80
CHEMBL3963350 1 7.50
CHEMBL3919677 1 7.44
CHEMBL3927051 1 7.43
CHEMBL3913586 1 6.75
CHEMBL3962874 1 6.49
CHEMBL3914119 1 6.39
CHEMBL3977219 1 6.36
CHEMBL3890510 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4542380 IC50 = 3.0 nM 8.52
CHEMBL4060831 IC50 = 9.0 nM 8.05
CHEMBL3938760 IC50 = 13.0 nM 7.89
CHEMBL3958947 IC50 = 16.0 nM 7.80
CHEMBL3963350 IC50 = 32.0 nM 7.50
CHEMBL3919677 IC50 = 36.0 nM 7.44
CHEMBL3927051 IC50 = 37.0 nM 7.43
CHEMBL3913586 IC50 = 180.0 nM 6.75
CHEMBL3962874 IC50 = 327.0 nM 6.49
CHEMBL3914119 IC50 = 406.0 nM 6.39
CHEMBL3977219 IC50 = 435.0 nM 6.36
CHEMBL3890510 IC50 - -