BDBM50050549 GSK2140944::Gepotidacin

SMILES c1c2c(cnc1CNC3CCN(CC3)C[C@@H]4CN5C(=O)C=CC6=C5N4C(=O)C=N6)OCCC2

InChI Key InChIKey=PZFAZQUREQIODZ-UHFFFAOYSA-N

Data  21 IC50

PDB links: 5 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 21 hits for monomerid = 50050549   

TargetDNA gyrase subunit A/B(Staphylococcus aureus)
National Institute of Chemistry

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 374nMAssay Description:Inhibition of Staphylococcus aureus DNA gyrase assessed as reduction in DNA supercoiling using relaxed pNO1 plasmid DNA as substrate incubated for 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 8.30E+3nMAssay Description:Inhibition of Staphylococcus aureus DNA topoisomerase 4 relaxation activity measured for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 244nMAssay Description:Inhibition of Escherichia coli DNA gyrase supercoiling incubated for 30 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 374nMAssay Description:Inhibition of Staphylococcus aureus DNA gyrase supercoiling incubated for 30 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.40E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetDNA topoisomerase 2-alpha(Human)
Redx Anti-Infectives

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 5.52E+4nMAssay Description:Inhibition of human topoisomerase 2 assessed as reduction in decatenationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of human ERG by Ionworks electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetDNA gyrase A/A/B/B tetramer(Escherichia coli (strain K12))
Redx Anti-Infectives

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 60nMAssay Description:Inhibition of Escherichia coli DNA gyrase supercoiling activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 4 subunit A/B(Staphylococcus aureus)
The Ohio State University

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of Staphylococcus aureus topoisomerase IV decatenation activity using kDNA as substrate by ethidium bromide/bromophenol blue staining base...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMed
TargetDNA gyrase subunit A/B(Staphylococcus aureus)
National Institute of Chemistry

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 170nMAssay Description:Inhibition of Staphylococcus aureus Gyrase supercoiling activity assessed as reduction in supercoiling pBR322 DNA by measuring relaxation by bromophe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 4 subunit A/B(Staphylococcus aureus)
The Ohio State University

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 8.30E+3nMAssay Description:Inhibition of Staphylococcus aureus topoisomerase 4 assessed as reduction in decatenation using supercoiled pNO1 plasmid DNA as substrate incubated f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.40E+6nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2016
Entry Details Article
PubMed
TargetDNA gyrase subunit A/B(Staphylococcus aureus)
National Institute of Chemistry

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 244nMAssay Description:Inhibition of Escherichia coli DNA gyrase assessed as reduction in DNA supercoiling using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA gyrase subunit A/B(Staphylococcus aureus)
National Institute of Chemistry

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 47nMAssay Description:Inhibition of Staphylococcus aureus DNA gyrase using positively supercoiled pBR322 DNA as substrate incubated for 25 mins by ethidium bromide stainin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.31E+6nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.40E+6nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetDNA gyrase subunit A/B(Staphylococcus aureus)
National Institute of Chemistry

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 47nMAssay Description:Inhibition of Staphylococcus aureus DNA gyraseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 4 subunit A/B(Staphylococcus aureus)
The Ohio State University

Curated by ChEMBL
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 600nMAssay Description:Inhibition of Staphylococcus aureus DNA topoisomerase 4More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.31E+6nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2019
Entry Details Article
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.31E+6nMAssay Description:Inhibition of human ERG expressed in CHO cells using -80 mV holding potential measured after 3 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM50050549(GSK2140944 | Gepotidacin)
Affinity DataIC50: 1.40E+6nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/4/2016
Entry Details Article
PubMed