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Assay Detail

CHEMBL2350642

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

Binding
Inhibition of PRMT3 (unknown origin) using [3H]SAM assessed as inhibition of biotinylated-H4 (1 to 24 amino acid residues) methylation after 1 hr by scintillation proximity assay
2
Total Activities
1
Compounds Tested
2
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 3 (CHEMBL5891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH, Vedadi M, Brown PJ, Schapira M.
Bioorg Med Chem (2013) 21 : 1787 -1794
PubMed 23433670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.94 5.94
IC50 1 5.64 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349526 2 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349526 Ki = 1150.0 nM 5.94
CHEMBL2349526 IC50 = 2300.0 nM 5.64