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Assay Detail

CHEMBL4810081

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

Binding
Inhibition of human NNMT expressed in HEK293 cells assessed as reduction in 1-methyl-nicotinamide formation measured after 24 hrs by RapidFire Mass spectroscopy
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell.
Hayashi K, Uehara S, Yamamoto S, Cary DR, Nishikawa J, Ueda T, Ozasa H, Mihara K, Yoshimura N, Kawai T, Ono T, Yamamoto S, Fumoto M, Mikamiyama H.
ACS Med Chem Lett (2021) 12 : 1093 -1101
PubMed 34267879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.77 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4872872 1 6.11
CHEMBL4859806 1 5.43
CHEMBL4868588 1 -
CHEMBL4867273 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4872872 IC50 = 770.0 nM 6.11
CHEMBL4859806 IC50 = 3700.0 nM 5.43
CHEMBL4868588 IC50 > 100000.0 nM -
CHEMBL4867273 IC50 > 100000.0 nM -