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Assay Detail

CHEMBL5364211

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

Binding
Binding affinity to full-length wild-type human NNMT (1 to 270 residues) expressed in Escherichia coli BL21(DE3) cells assessed as apparent inhibition constant preincubated for 30 mins followed by nicotinamide addition by fluorescence-based SAHH-coupled assay
3
Total Activities
3
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

Nicotinamide N-methyltransferase (CHEMBL2346486)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship Studies on Cell-Potent Nicotinamide <i>N</i>-Methyltransferase Bisubstrate Inhibitors.
Iyamu ID, Zhao T, Huang R.
J Med Chem (2023) 66 : 10510 -10527
PubMed 37523719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.65 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5408922 1 8.92
CHEMBL5433732 1 8.80
CHEMBL5420435 1 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5408922 Ki = 1.2 nM 8.92
CHEMBL5433732 Ki = 1.6 nM 8.80
CHEMBL5420435 Ki = 5.9 nM 8.23