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Assay Detail

CHEMBL5675948

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

Binding
Inhibition of SMYD2 (unknown origin) using N-terminal GST-tagged MAP3K2 and 3H-SAM as substrate for 2 hrs by TopCount NXT plate reader
4
Total Activities
4
Compounds Tested
1
Activity Types
2
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

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA.
PLoS One (2018) 13 : 197372 -197372
PubMed 29856759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.82 8.41

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187983 1 8.41
CHEMBL5197760 1 7.80
CHEMBL3414623 1 7.77
CHEMBL2169920 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187983 IC50 = 3.9 nM 8.41
CHEMBL5197760 IC50 = 16.0 nM 7.80
CHEMBL3414623 IC50 = 17.0 nM 7.77
CHEMBL2169920 IC50 = 51.0 nM 7.29