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Assay Detail

CHEMBL2422986

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Functional
Inhibition of protein synthesis in Escherichia coli S30 extracts after 90 mins by coupled transcription/translation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Escherichia coli
Confidence 1 — Organism
Curated By Autocuration

Target

Escherichia coli (CHEMBL354)
Type ORGANISM
Organism Escherichia coli

Publication

Synthesis and evaluation of hetero- and homodimers of ribosome-targeting antibiotics: antimicrobial activity, in vitro inhibition of translation, and drug resistance.
Berkov-Zrihen Y, Green KD, Labby KJ, Feldman M, Garneau-Tsodikova S, Fridman M.
J Med Chem (2013) 56 : 5613 -5625
PubMed 23786357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.48 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1747 TOBRAMYCIN 4.0 1 7.82
CHEMBL2417987 1 6.57
CHEMBL2418138 1 6.37
CHEMBL2417984 1 6.01
CHEMBL2417982 1 6.00
CHEMBL2417983 1 5.83
CHEMBL2417988 1 5.21
CHEMBL130 CHLORAMPHENICOL 4.0 1 5.19
CHEMBL2417981 1 4.83
CHEMBL2417980 1 4.74
CHEMBL1753 CLINDAMYCIN 4.0 1 4.74
CHEMBL2417985 1 4.59
CHEMBL2417986 1 4.48
CHEMBL2417989 1 4.31
CHEMBL2418137 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1747 TOBRAMYCIN IC50 = 15.0 nM 7.82
CHEMBL2417987 IC50 = 270.0 nM 6.57
CHEMBL2418138 IC50 = 430.0 nM 6.37
CHEMBL2417984 IC50 = 980.0 nM 6.01
CHEMBL2417982 IC50 = 1000.0 nM 6.00
CHEMBL2417983 IC50 = 1490.0 nM 5.83
CHEMBL2417988 IC50 = 6100.0 nM 5.21
CHEMBL130 CHLORAMPHENICOL IC50 = 6400.0 nM 5.19
CHEMBL2417981 IC50 = 14700.0 nM 4.83
CHEMBL2417980 IC50 = 18300.0 nM 4.74
CHEMBL1753 CLINDAMYCIN IC50 = 18100.0 nM 4.74
CHEMBL2417985 IC50 = 25600.0 nM 4.59
CHEMBL2417986 IC50 = 32900.0 nM 4.48
CHEMBL2417989 IC50 = 48700.0 nM 4.31
CHEMBL2418137 IC50 > 100000.0 nM -