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Assay Detail

CHEMBL5720044

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

Binding
Binding affinity to human PRMT4 assessed as inhibition constant using (3H) methylated biotin labelled peptide as substrate in presence of 3H-SAM by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
2
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

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
Eram MS, Shen Y, Szewczyk M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C, Dong A, Zeng H, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J.
ACS Chem Biol (2016) 11 : 772 -781
PubMed 26598975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.28 7.64

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3901808 1 7.64
CHEMBL5722978 1 6.92
CHEMBL5722993 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3901808 Ki = 23.0 nM 7.64
CHEMBL5722978 Ki = 120.0 nM 6.92
CHEMBL5722993 Ki > 37500.0 nM -