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Assay Detail

CHEMBL4137482

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

Binding
Competitive inhibition of human G9a using 40 to 2560 nM biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay
2
Total Activities
2
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

Histone-lysine N-methyltransferase EHMT2 (CHEMBL6032)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
Rabal O, San José-Enériz E, Agirre X, Sánchez-Arias JA, Vilas-Zornoza A, Ugarte A, de Miguel I, Miranda E, Garate L, Fraga M, Santamarina P, Fernandez Perez R, Ordoñez R, Sáez E, Roa S, García-Barchino MJ, Martínez-Climent JA, Liu Y, Wu W, Xu M, Prosper F, Oyarzabal J.
J Med Chem (2018) 61 : 6518 -6545
PubMed 29953809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.15 9.15
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162206 1 9.15
CHEMBL4170225 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162206 IC50 = 0.7 nM 9.15
CHEMBL4170225 Inhibition - % -