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Assay Detail

CHEMBL748919

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

Binding
Inhibition of human N-myristoyltransferase (NMT)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Conformationally constrained [p-(omega-aminoalkyl)phenacetyl]-L-seryl-L-lysyl dipeptide amides as potent peptidomimetic inhibitors of Candida albicans and human myristoyl-CoA:protein N-myristoyl transferase.
Nagarajan SR, Devadas B, Zupec ME, Freeman SK, Brown DL, Lu HF, Mehta PP, Kishore NS, McWherter CA, Getman DP, Gordon JI, Sikorski JA.
J Med Chem (1997) 40 : 1422 -1438
PubMed 9154965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.73 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286570 1 6.38
CHEMBL33289 1 6.30
CHEMBL33525 1 6.12
CHEMBL34342 1 6.10
CHEMBL33664 1 6.10
CHEMBL416405 1 6.00
CHEMBL33572 1 5.94
CHEMBL33856 1 5.82
CHEMBL285198 1 5.75
CHEMBL285000 1 4.28
CHEMBL33668 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286570 IC50 = 420.0 nM 6.38
CHEMBL33289 IC50 = 500.0 nM 6.30
CHEMBL33525 IC50 = 760.0 nM 6.12
CHEMBL34342 IC50 = 790.0 nM 6.10
CHEMBL33664 IC50 = 800.0 nM 6.10
CHEMBL416405 IC50 = 990.0 nM 6.00
CHEMBL33572 IC50 = 1140.0 nM 5.94
CHEMBL33856 IC50 = 1500.0 nM 5.82
CHEMBL285198 IC50 = 1800.0 nM 5.75
CHEMBL285000 IC50 = 53000.0 nM 4.28
CHEMBL33668 IC50 = 62000.0 nM 4.21