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Assay Detail

CHEMBL1228353

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Functional
Inhibition of protein synthesis in human HeLa cells assessed as [35S]cysteine/methionine utilization after 2 hrs by scintillation spectroscopy
12
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Inhibition of eukaryotic translation elongation by cycloheximide and lactimidomycin.
Schneider-Poetsch T, Ju J, Eyler DE, Dang Y, Bhat S, Merrick WC, Green R, Shen B, Liu JO.
Nat Chem Biol (2010) 6 : 209 -217
PubMed 20118940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 6 - -
IC50 6 6.49 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1221911 LACTIMIDOMYCIN 2 7.42
CHEMBL1222014 2H LACTIMIDOMYCIN K 1 7.01
CHEMBL1554 DACTINOMYCIN 4.0 2 6.28
CHEMBL123292 CYCLOHEXIMIDE 2.0 2 6.27
CHEMBL1221912 ISOMIGRASTATIN 2 6.21
CHEMBL1222015 DIDEHYDRO ISOMIGRASTATIN 1 5.72
CHEMBL474321 MIGRASTATIN 1 -
CHEMBL1221965 DORRIGOCIN B 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1221911 LACTIMIDOMYCIN IC50 = 37.82 nM 7.42
CHEMBL1222014 2H LACTIMIDOMYCIN K IC50 = 98.47 nM 7.01
CHEMBL1554 DACTINOMYCIN IC50 = 519.7 nM 6.28
CHEMBL123292 CYCLOHEXIMIDE IC50 = 532.5 nM 6.27
CHEMBL1221912 ISOMIGRASTATIN IC50 = 624.0 nM 6.21
CHEMBL1222015 DIDEHYDRO ISOMIGRASTATIN IC50 = 1909.0 nM 5.72
CHEMBL123292 CYCLOHEXIMIDE Inhibition - % -
CHEMBL1554 DACTINOMYCIN Inhibition - % -
CHEMBL1221912 ISOMIGRASTATIN Inhibition - % -
CHEMBL1221911 LACTIMIDOMYCIN Inhibition - % -
CHEMBL474321 MIGRASTATIN Inhibition - % -
CHEMBL1221965 DORRIGOCIN B Inhibition - % -