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Assay Detail

CHEMBL744118

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

Binding
Inhibition activity against N-myristoyltransferase (NMT) of human.
16
Total Activities
16
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

Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.
Devadas B, Freeman SK, Zupec ME, Lu HF, Nagarajan SR, Kishore NS, Lodge JK, Kuneman DW, McWherter CA, Vinjamoori DV, Getman DP, Gordon JI, Sikorski JA.
J Med Chem (1997) 40 : 2609 -2625
PubMed 9258368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.04 6.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291811 1 6.31
CHEMBL59835 1 5.81
CHEMBL188653 1 5.10
CHEMBL291791 1 5.09
CHEMBL299249 1 4.95
CHEMBL6269 SC-58272 1 4.85
CHEMBL294596 1 4.80
CHEMBL89727 1 4.64
CHEMBL88093 1 4.55
CHEMBL62081 1 4.31
CHEMBL91048 1 -
CHEMBL313084 1 -
CHEMBL313161 1 -
CHEMBL86687 1 -
CHEMBL89452 1 -
CHEMBL86856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291811 IC50 = 490.0 nM 6.31
CHEMBL59835 IC50 = 1540.0 nM 5.81
CHEMBL188653 IC50 = 8000.0 nM 5.10
CHEMBL291791 IC50 = 8200.0 nM 5.09
CHEMBL299249 IC50 = 11350.0 nM 4.95
CHEMBL6269 SC-58272 IC50 = 14100.0 nM 4.85
CHEMBL294596 IC50 = 16000.0 nM 4.80
CHEMBL89727 IC50 = 22700.0 nM 4.64
CHEMBL88093 IC50 = 28200.0 nM 4.55
CHEMBL62081 IC50 = 49000.0 nM 4.31
CHEMBL91048 IC50 = 142000.0 nM -
CHEMBL313084 IC50 = 119500.0 nM -
CHEMBL313161 IC50 = 809500.0 nM -
CHEMBL86687 IC50 > 1000000.0 nM -
CHEMBL89452 IC50 > 100000.0 nM -
CHEMBL86856 IC50 = 840000.0 nM -