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Assay Detail

CHEMBL4479555

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

Binding
Inhibition of PRMT5 (unknown origin)
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 5 (CHEMBL1795116)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV.
Bioorg Med Chem Lett (2016) 26 : 4518 -4522
PubMed 27485386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.16 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE 1 6.70
CHEMBL4588797 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE IC50 = 200.0 nM 6.70
CHEMBL4588797 IC50 = 2400.0 nM 5.62