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Assay Detail

CHEMBL5366083

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

Binding
Inhibition of N-terminal/C-terminal His-tagged human recombinant full-length PRMT7 (2 to 692 residues) using histone GST-GAR as substrate and 3H-SAM as cosubstrate incubated for 60 mins by scintillation counter analysis
2
Total Activities
2
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 7 (CHEMBL3562175)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.
Feoli A, Iannelli G, Cipriano A, Milite C, Shen L, Wang Z, Hadjikyriacou A, Lowe TL, Safaeipour C, Viviano M, Sarno G, Morretta E, Monti MC, Yang Y, Clarke SG, Cosconati S, Castellano S, Sbardella G.
J Med Chem (2023) 66 : 13665 -13683
PubMed 37560786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.76 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5408585 1 6.27
CHEMBL5396270 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5408585 IC50 = 540.0 nM 6.27
CHEMBL5396270 IC50 = 5600.0 nM 5.25