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Assay Detail

CHEMBL906490

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Functional
Inhibition of protein synthesis in Escherichia coli by coupled transcription-translation assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Escherichia coli (CHEMBL354)
Type ORGANISM
Organism Escherichia coli

Publication

Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics.
Zhou Y, Gregor VE, Ayida BK, Winters GC, Sun Z, Murphy D, Haley G, Bailey D, Froelich JM, Fish S, Webber SE, Hermann T, Wall D.
Bioorg Med Chem Lett (2007) 17 : 1206 -1210
PubMed 17188860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 4.91 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1384 KANAMYCIN 4.0 1 6.40
CHEMBL396495 1 6.00
CHEMBL441212 1 6.00
CHEMBL130 CHLORAMPHENICOL 4.0 1 5.82
CHEMBL1440 TETRACYCLINE 4.0 1 5.55
CHEMBL387427 1 5.52
CHEMBL231613 1 5.30
CHEMBL374035 1 5.16
CHEMBL231513 1 5.16
CHEMBL218010 1 5.16
CHEMBL398198 1 5.10
CHEMBL397680 1 5.10
CHEMBL398199 1 5.10
CHEMBL231021 1 5.00
CHEMBL449044 1 5.00
CHEMBL396255 1 5.00
CHEMBL219806 1 5.00
CHEMBL231332 1 4.96
CHEMBL398200 1 4.96
CHEMBL415671 1 4.92
CHEMBL388647 1 4.89
CHEMBL396518 1 4.89
CHEMBL230512 1 4.85
CHEMBL397510 1 4.82
CHEMBL230046 1 4.80
CHEMBL388424 1 4.77
CHEMBL388423 1 4.77
CHEMBL230154 1 4.75
CHEMBL231228 1 4.72
CHEMBL230157 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1384 KANAMYCIN IC50 = 400.0 nM 6.40
CHEMBL396495 IC50 = 1000.0 nM 6.00
CHEMBL441212 IC50 = 1000.0 nM 6.00
CHEMBL130 CHLORAMPHENICOL IC50 = 1500.0 nM 5.82
CHEMBL1440 TETRACYCLINE IC50 = 2800.0 nM 5.55
CHEMBL387427 IC50 = 3000.0 nM 5.52
CHEMBL231613 IC50 = 5000.0 nM 5.30
CHEMBL374035 IC50 = 7000.0 nM 5.16
CHEMBL231513 IC50 = 7000.0 nM 5.16
CHEMBL218010 IC50 = 7000.0 nM 5.16
CHEMBL398198 IC50 = 8000.0 nM 5.10
CHEMBL397680 IC50 = 8000.0 nM 5.10
CHEMBL398199 IC50 = 8000.0 nM 5.10
CHEMBL219806 IC50 = 10000.0 nM 5.00
CHEMBL449044 IC50 = 10000.0 nM 5.00
CHEMBL231021 IC50 = 10000.0 nM 5.00
CHEMBL396255 IC50 = 10000.0 nM 5.00
CHEMBL231332 IC50 = 11000.0 nM 4.96
CHEMBL398200 IC50 = 11000.0 nM 4.96
CHEMBL415671 IC50 = 12000.0 nM 4.92
CHEMBL388647 IC50 = 13000.0 nM 4.89
CHEMBL396518 IC50 = 13000.0 nM 4.89
CHEMBL230512 IC50 = 14000.0 nM 4.85
CHEMBL397510 IC50 = 15000.0 nM 4.82
CHEMBL230046 IC50 = 16000.0 nM 4.80
CHEMBL388423 IC50 = 17000.0 nM 4.77
CHEMBL388424 IC50 = 17000.0 nM 4.77
CHEMBL230154 IC50 = 18000.0 nM 4.75
CHEMBL231228 IC50 = 19000.0 nM 4.72
CHEMBL230157 IC50 = 19000.0 nM 4.72
CHEMBL397748 IC50 = 21000.0 nM 4.68
CHEMBL231231 IC50 = 21000.0 nM 4.68
CHEMBL231330 IC50 = 27000.0 nM 4.57
CHEMBL387798 IC50 = 31000.0 nM 4.51
CHEMBL230917 IC50 = 36000.0 nM 4.44
CHEMBL231229 IC50 = 40000.0 nM 4.40
CHEMBL387586 IC50 = 40000.0 nM 4.40
CHEMBL231331 IC50 = 43000.0 nM 4.37
CHEMBL231230 IC50 = 44000.0 nM 4.36
CHEMBL389084 IC50 = 58000.0 nM 4.24
CHEMBL440968 IC50 = 72000.0 nM 4.14
CHEMBL276220 IC50 = 77000.0 nM 4.11
CHEMBL395260 IC50 = 100000.0 nM 4.00
CHEMBL231022 IC50 = 310000.0 nM -
CHEMBL398197 IC50 = 800000.0 nM -
CHEMBL230045 IC50 > 1000000.0 nM -
CHEMBL230513 IC50 > 1000000.0 nM -
CHEMBL231187 IC50 > 1000000.0 nM -