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Assay Detail

CHEMBL3420959

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

Binding
Inhibition of human SETD2 (1347 to 1711) using histamine H3 (20 to 50) as substrate assessed as transfer of [3H]-Me of [3H-Me]-SAM to peptide substrate after 4 hrs by scintillation counting analysis
1
Total Activities
1
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-lysine N-methyltransferase SETD2 (CHEMBL3108647)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibitors of protein methyltransferases.
Kaniskan HÜ, Konze KD, Jin J.
J Med Chem (2015) 58 : 1596 -1629
PubMed 25406853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.10 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414624 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414624 IC50 = 800.0 nM 6.10