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Assay Detail

CHEMBL744115

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

Binding
Tested for Inhibitory concentration against human N-myristoyltransferase (NMT) in radiochemical HPLC end point assay with peptide GNAASARR-NH2 and [3H]myristoyl-CoA radioligand at 1 uM
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Peptide N-myristoyltransferase (CHEMBL2096973)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Replacements for lysine in l-seryl-l-lysyl dipeptide amide inhibitors of candida albicans myristoyl-CoA:protein N-myristoyltransferase
Brown DL, Devadas B, Lu H, Nagarajan S, Zupec ME, Freeman SK, McWherter CA, Getman DP, Sikorski JA
Bioorg Med Chem Lett (1997) 7 : 379 -382
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.12 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33289 1 6.30
CHEMBL331272 1 6.00
CHEMBL6269 SC-58272 1 4.85
CHEMBL279641 1 4.76
CHEMBL341147 1 4.54
CHEMBL125031 1 4.28
CHEMBL340659 1 -
CHEMBL124696 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33289 IC50 = 500.0 nM 6.30
CHEMBL331272 IC50 = 1000.0 nM 6.00
CHEMBL6269 SC-58272 IC50 = 14100.0 nM 4.85
CHEMBL279641 IC50 = 17200.0 nM 4.76
CHEMBL341147 IC50 = 29000.0 nM 4.54
CHEMBL125031 IC50 = 52000.0 nM 4.28
CHEMBL340659 IC50 >= 200000.0 nM -
CHEMBL124696 IC50 > 10000.0 nM -