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Assay Detail

CHEMBL5138963

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

Binding
Binding affinity to full length recombinant PRMT4 (unknown origin) assessed as dissociation constant by surface plasmon resonance
9
Total Activities
9
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

Histone-arginine methyltransferase CARM1 (CHEMBL5406)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.
Iannelli G, Milite C, Marechal N, Cura V, Bonnefond L, Troffer-Charlier N, Feoli A, Rescigno D, Wang Y, Cipriano A, Viviano M, Bedford MT, Cavarelli J, Castellano S, Sbardella G.
J Med Chem (2022) 65 : 11574 -11606
PubMed 35482954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 6.56 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5172334 1 8.02
CHEMBL5191769 1 7.29
CHEMBL5173678 1 7.12
CHEMBL5202088 1 6.60
CHEMBL5206272 1 6.45
CHEMBL5186617 1 6.22
CHEMBL5199380 1 6.18
CHEMBL5170047 1 5.64
CHEMBL5180108 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5172334 Kd = 9.6 nM 8.02
CHEMBL5191769 Kd = 51.7 nM 7.29
CHEMBL5173678 Kd = 75.9 nM 7.12
CHEMBL5202088 Kd = 252.0 nM 6.60
CHEMBL5206272 Kd = 359.2 nM 6.45
CHEMBL5186617 Kd = 603.4 nM 6.22
CHEMBL5199380 Kd = 663.4 nM 6.18
CHEMBL5170047 Kd = 2300.0 nM 5.64
CHEMBL5180108 Kd = 2800.0 nM 5.55