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Assay Detail

CHEMBL2330189

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

Binding
Inhibition of Escherichia coli HldE-kinase preincubated for 30 mins prior to substrate addition measured after 30 mins by luminescence assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Vectorization efforts to increase Gram-negative intracellular drug concentration: a case study on HldE-K inhibitors.
Atamanyuk D, Faivre F, Oxoby M, Ledoussal B, Drocourt E, Moreau F, Gerusz V.
J Med Chem (2013) 56 : 1908 -1921
PubMed 23445125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.92 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325152 1 9.00
CHEMBL2325156 1 7.80
CHEMBL2312560 1 7.72
CHEMBL2325159 1 7.60
CHEMBL2325158 1 7.52
CHEMBL2325155 1 7.48
CHEMBL2325142 1 7.26
CHEMBL2325154 1 7.16
CHEMBL2325157 1 7.15
CHEMBL2325144 1 7.09
CHEMBL2325141 1 7.01
CHEMBL2325147 1 6.96
CHEMBL2325148 1 6.96
CHEMBL2325139 1 6.38
CHEMBL2325149 1 6.29
CHEMBL2325153 1 6.28
CHEMBL2325150 1 6.24
CHEMBL2325151 1 6.20
CHEMBL2325140 1 6.18
CHEMBL2325143 1 6.11
CHEMBL2325145 1 6.06
CHEMBL2325146 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325152 IC50 = 1.0 nM 9.00
CHEMBL2325156 IC50 = 16.0 nM 7.80
CHEMBL2312560 IC50 = 19.0 nM 7.72
CHEMBL2325159 IC50 = 25.0 nM 7.60
CHEMBL2325158 IC50 = 30.0 nM 7.52
CHEMBL2325155 IC50 = 33.0 nM 7.48
CHEMBL2325142 IC50 = 55.0 nM 7.26
CHEMBL2325154 IC50 = 69.0 nM 7.16
CHEMBL2325157 IC50 = 71.0 nM 7.15
CHEMBL2325144 IC50 = 82.0 nM 7.09
CHEMBL2325141 IC50 = 98.0 nM 7.01
CHEMBL2325147 IC50 = 110.0 nM 6.96
CHEMBL2325148 IC50 = 110.0 nM 6.96
CHEMBL2325139 IC50 = 420.0 nM 6.38
CHEMBL2325149 IC50 = 510.0 nM 6.29
CHEMBL2325153 IC50 = 520.0 nM 6.28
CHEMBL2325150 IC50 = 580.0 nM 6.24
CHEMBL2325151 IC50 = 630.0 nM 6.20
CHEMBL2325140 IC50 = 660.0 nM 6.18
CHEMBL2325143 IC50 = 780.0 nM 6.11
CHEMBL2325145 IC50 = 880.0 nM 6.06
CHEMBL2325146 IC50 = 1400.0 nM 5.85