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Assay Detail

CHEMBL4199784

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

Binding
Inhibition of recombinant human Cx26 expressed in Escherichia coli LB2003 assessed as reduction in cell growth measured after 18 hrs
29
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Gap junction beta-2 protein (CHEMBL4295738)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of Connexin Hemichannels by New Amphiphilic Aminoglycosides without Antibiotic Activity.
AlFindee MN, Subedi YP, Fiori MC, Krishnan S, Kjellgren A, Altenberg GA, Chang CT.
ACS Med Chem Lett (2018) 9 : 697 -701
PubMed 30034603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.09 5.60
Imax 14 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204676 2 5.60
CHEMBL4205159 2 5.37
CHEMBL4209017 2 5.31
CHEMBL4210911 2 5.21
CHEMBL4213413 2 5.21
CHEMBL4213933 2 5.18
CHEMBL4203134 2 5.12
CHEMBL4209535 2 5.09
CHEMBL4212437 2 5.08
CHEMBL1384 KANAMYCIN 4.0 1 5.03
CHEMBL4216863 2 4.89
CHEMBL4215327 2 4.87
CHEMBL4210382 2 4.87
CHEMBL4214786 2 4.73
CHEMBL4206024 2 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204676 IC50 = 2500.0 nM 5.60
CHEMBL4205159 IC50 = 4300.0 nM 5.37
CHEMBL4209017 IC50 = 4900.0 nM 5.31
CHEMBL4210911 IC50 = 6200.0 nM 5.21
CHEMBL4213413 IC50 = 6200.0 nM 5.21
CHEMBL4213933 IC50 = 6600.0 nM 5.18
CHEMBL4203134 IC50 = 7600.0 nM 5.12
CHEMBL4209535 IC50 = 8100.0 nM 5.09
CHEMBL4212437 IC50 = 8400.0 nM 5.08
CHEMBL1384 KANAMYCIN IC50 = 9400.0 nM 5.03
CHEMBL4216863 IC50 = 13000.0 nM 4.89
CHEMBL4215327 IC50 = 13600.0 nM 4.87
CHEMBL4210382 IC50 = 13500.0 nM 4.87
CHEMBL4214786 IC50 = 18800.0 nM 4.73
CHEMBL4206024 IC50 = 19000.0 nM 4.72
CHEMBL4204676 Imax = 94.0 % -
CHEMBL4213413 Imax = 94.0 % -
CHEMBL4205159 Imax = 94.0 % -
CHEMBL4209535 Imax = 94.0 % -
CHEMBL4209017 Imax = 94.0 % -
CHEMBL4213933 Imax = 94.0 % -
CHEMBL4214786 Imax = 99.0 % -
CHEMBL4216863 Imax = 94.0 % -
CHEMBL4212437 Imax = 99.0 % -
CHEMBL4203134 Imax = 99.0 % -
CHEMBL4206024 Imax = 99.0 % -
CHEMBL4210911 Imax = 99.0 % -
CHEMBL4210382 Imax = 99.0 % -
CHEMBL4215327 Imax = 99.0 % -