Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4147359

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

Binding
Inhibition of bacterial C-terminal His6-tagged ErmC' (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as decrease in rRNA methylation using [methyl-3H]AdoMet measured after 1 hr
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacteria
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

rRNA adenine N-6-methyltransferase (CHEMBL4295568)
Type SINGLE PROTEIN
Organism Staphylococcus aureus (strain N315)

Publication

Novel inhibitors of the rRNA ErmC' methyltransferase to block resistance to macrolides, lincosamides, streptogramine B antibiotics.
Foik IP, Tuszynska I, Feder M, Purta E, Stefaniak F, Bujnicki JM.
Eur J Med Chem (2018) 146 : 60 -67
PubMed 29396363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 4.00 4.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4172068 1 4.00
CHEMBL4164894 1 -
CHEMBL4176470 1 -
CHEMBL4166273 1 -
CHEMBL4159029 1 -
CHEMBL4169684 1 -
CHEMBL2273057 1 -
CHEMBL4159457 1 -
CHEMBL4166678 1 -
CHEMBL4175957 1 -
CHEMBL4168106 1 -
CHEMBL4172554 1 -
CHEMBL4165617 1 -
CHEMBL4162181 1 -
CHEMBL4171668 1 -
CHEMBL4161475 1 -
CHEMBL4175510 1 -
CHEMBL4168166 1 -
CHEMBL4168716 1 -
CHEMBL4174185 1 -
CHEMBL4098242 1 -
CHEMBL4162356 1 -
CHEMBL4173033 1 -
CHEMBL4165804 1 -
CHEMBL4176416 1 -
CHEMBL4169237 1 -
CHEMBL4161309 1 -
CHEMBL4172623 1 -
CHEMBL4164726 1 -
CHEMBL4173217 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4172068 IC50 = 100000.0 nM 4.00
CHEMBL4176016 IC50 > 500000.0 nM -
CHEMBL4159457 IC50 > 250000.0 nM -
CHEMBL2273057 IC50 = 500000.0 nM -
CHEMBL4169684 IC50 = 500000.0 nM -
CHEMBL4159029 IC50 = 250000.0 nM -
CHEMBL4166273 IC50 = 500000.0 nM -
CHEMBL4176470 IC50 = 500000.0 nM -
CHEMBL4165860 IC50 = 250000.0 nM -
CHEMBL4176579 IC50 > 500000.0 nM -
CHEMBL4165307 IC50 = 500000.0 nM -
CHEMBL4163790 IC50 > 500000.0 nM -
CHEMBL4175957 IC50 - -
CHEMBL4177311 IC50 = 110000.0 nM -
CHEMBL4170092 IC50 > 500000.0 nM -
CHEMBL4173546 IC50 > 500000.0 nM -
CHEMBL4176909 IC50 > 500000.0 nM -
CHEMBL4169047 IC50 = 500000.0 nM -
CHEMBL4161776 IC50 > 500000.0 nM -
CHEMBL4172416 IC50 > 500000.0 nM -
CHEMBL4164668 IC50 > 500000.0 nM -
CHEMBL4162820 IC50 > 500000.0 nM -
CHEMBL4170758 IC50 > 250000.0 nM -
CHEMBL4174185 IC50 - -
CHEMBL4173217 IC50 - -
CHEMBL4164726 IC50 > 500000.0 nM -
CHEMBL4172623 IC50 = 250000.0 nM -
CHEMBL4161309 IC50 = 500000.0 nM -
CHEMBL4169237 IC50 > 500000.0 nM -
CHEMBL4176416 IC50 > 500000.0 nM -
CHEMBL4165804 IC50 = 250000.0 nM -
CHEMBL4173033 IC50 > 500000.0 nM -
CHEMBL4162356 IC50 > 500000.0 nM -
CHEMBL4098242 IC50 = 299000.0 nM -
CHEMBL4166678 IC50 = 116000.0 nM -
CHEMBL4168716 IC50 - -
CHEMBL4168166 IC50 = 500000.0 nM -
CHEMBL4175510 IC50 - -
CHEMBL4164894 IC50 - -
CHEMBL4161475 IC50 - -
CHEMBL4171668 IC50 - -
CHEMBL4162181 IC50 - -
CHEMBL4165617 IC50 - -
CHEMBL4172554 IC50 - -
CHEMBL4168106 IC50 - -