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Assay Detail

CHEMBL4772325

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

Binding
Inhibition of human Cx26 expressed in Escherichia coli LB2003 cells in medium containing 4 mM K+ and 500 uM IPTG by measuring cell growth after 18 hrs by plate reader
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Amphiphilic aminoglycosides with increased selectivity for inhibition of connexin 43 (Cx43) hemichannels.
Subedi YP,Kjellgren A,Roberts P,Montgomery H,Thackeray N,Fiori MC,Altenberg GA,Chang CT
Eur J Med Chem (2020) 203 : 112602 -112602
PubMed 32679454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.72 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4780949 1 5.22
CHEMBL1384 KANAMYCIN 4.0 1 4.94
CHEMBL4785499 1 4.90
CHEMBL4776897 1 4.76
CHEMBL4799209 1 4.73
CHEMBL4790312 1 4.31
CHEMBL4795796 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4780949 IC50 = 6000.0 nM 5.22
CHEMBL1384 KANAMYCIN IC50 = 11500.0 nM 4.94
CHEMBL4785499 IC50 = 12700.0 nM 4.90
CHEMBL4776897 IC50 = 17200.0 nM 4.76
CHEMBL4799209 IC50 = 18600.0 nM 4.73
CHEMBL4790312 IC50 = 49400.0 nM 4.31
CHEMBL4795796 IC50 = 66700.0 nM 4.18