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Assay Detail

CHEMBL3821409

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Binding
Inhibition of SMYD2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using Biotinaminohexanoyl-GSRAHSSHLKSKKGQSTSRH as substrate after 75 mins by scintillation proximity assay
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

N-lysine methyltransferase SMYD2 (CHEMBL2169716)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C.
J Med Chem (2016) 59 : 4578 -4600
PubMed 27075367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.92 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2169920 1 6.92
CHEMBL3414623 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2169920 IC50 = 120.0 nM 6.92
CHEMBL3414623 IC50 < 15.0 nM -