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Assay Detail

CHEMBL1638698

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

Binding
Binding affinity to Escherichia coli ribosome assessed as inhibition of transcription-translational activity by luciferase assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Subcellular Ribosome
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Bacterial 70S ribosome (CHEMBL2363135)
Type PROTEIN NUCLEIC-ACID COMPLEX
Organism Bacteria

Publication

Second generation analogs of rigid 6,7-spiro scaffolds targeting the bacterial ribosome.
Stathakis CI, Mavridis I, Kythreoti G, Papakyriakou A, Katsoulis IA, Cottin T, Anastasopoulou P, Vourloumis D.
Bioorg Med Chem Lett (2010) 20 : 7488 -7492
PubMed 21041083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.44 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184618 FRAMYCETIN 3.0 1 7.50
CHEMBL427409 NEAMINE 1 5.30
CHEMBL1631490 1 4.95
CHEMBL1631496 1 4.01
CHEMBL1631491 1 -
CHEMBL1631492 1 -
CHEMBL1631493 1 -
CHEMBL1631494 1 -
CHEMBL1631495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184618 FRAMYCETIN IC50 = 32.0 nM 7.50
CHEMBL427409 NEAMINE IC50 = 5000.0 nM 5.30
CHEMBL1631490 IC50 = 11300.0 nM 4.95
CHEMBL1631496 IC50 = 98000.0 nM 4.01
CHEMBL1631491 IC50 = 168000.0 nM -
CHEMBL1631492 IC50 = 118000.0 nM -
CHEMBL1631493 IC50 > 1000000.0 nM -
CHEMBL1631494 IC50 = 429000.0 nM -
CHEMBL1631495 IC50 = 186000.0 nM -