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Assay Detail

CHEMBL4147367

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Binding
Inhibition of bacterial C-terminal His6-tagged ErmC' expressed in Escherichia coli BL21(DE3) assessed as decrease of protein binding to [gamma-33P]ATP-labeled 32-nt oligonucleotide after 30 mins by filter binding assay
2
Total Activities
2
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
Kd 2 6.69 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177311 1 7.40
CHEMBL4166678 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177311 Kd = 40.0 nM 7.40
CHEMBL4166678 Kd = 1040.0 nM 5.98