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Assay Detail

CHEMBL2215171

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Binding
Inhibition of ribosome-mediated protein synthesis in rabbit reticulocytes after 60 mins by coupled transcription/translation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Subcellular Ribosome
Confidence 2 — Organism
Curated By Autocuration

Target

Ribosome (CHEMBL613299)
Type SUBCELLULAR

Publication

Increased selectivity toward cytoplasmic versus mitochondrial ribosome confers improved efficiency of synthetic aminoglycosides in fixing damaged genes: a strategy for treatment of genetic diseases caused by nonsense mutations.
Kandasamy J, Atia-Glikin D, Shulman E, Shapira K, Shavit M, Belakhov V, Baasov T.
J Med Chem (2012) 55 : 10630 -10643
PubMed 23148581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.11 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206184 1 6.16
CHEMBL2206185 1 6.05
CHEMBL2206194 1 5.82
CHEMBL2206186 GENETICIN SULFATE SALT 1 5.70
CHEMBL2206189 1 5.55
CHEMBL2206193 1 5.34
CHEMBL2206192 1 5.28
CHEMBL2206195 1 5.10
CHEMBL2206190 1 4.80
CHEMBL2206188 1 4.77
CHEMBL2206187 1 4.62
CHEMBL2206191 1 4.55
CHEMBL373500 1 4.51
CHEMBL2206196 PAROMOMYCIN SULFATE 4.0 1 4.24
CHEMBL6067484 GENTAMICIN SULFATE 4.0 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206184 IC50 = 700.0 nM 6.16
CHEMBL2206185 IC50 = 900.0 nM 6.05
CHEMBL2206194 IC50 = 1500.0 nM 5.82
CHEMBL2206186 GENETICIN SULFATE SALT IC50 = 2000.0 nM 5.70
CHEMBL2206189 IC50 = 2800.0 nM 5.55
CHEMBL2206193 IC50 = 4600.0 nM 5.34
CHEMBL2206192 IC50 = 5200.0 nM 5.28
CHEMBL2206195 IC50 = 8000.0 nM 5.10
CHEMBL2206190 IC50 = 16000.0 nM 4.80
CHEMBL2206188 IC50 = 17000.0 nM 4.77
CHEMBL2206187 IC50 = 24000.0 nM 4.62
CHEMBL2206191 IC50 = 28000.0 nM 4.55
CHEMBL373500 IC50 = 31000.0 nM 4.51
CHEMBL2206196 PAROMOMYCIN SULFATE IC50 = 57000.0 nM 4.24
CHEMBL6067484 GENTAMICIN SULFATE IC50 = 62000.0 nM 4.21