ChEMBL ligand: CHEMBL3317856 (Gepotidacin, Gepotidacina, Gepotidacine, GSK-2140944, GSK2140944)
DNA gyrase subunit A/DNA gyrase subunit B/DNA gyrase in Escherichia coli [ChEMBL: CHEMBL2094139] [GtoPdb: 3217, 3218] [UniProtKB: P0AES4, P0AES6] DNA gyrase in S.aureus [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831] There should be some charts here, you may need to enable JavaScript!
DNA topoisomerase II alpha in Human [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] There should be some charts here, you may need to enable JavaScript!
Topoisomerase IV in S.aureus [ChEMBL: CHEMBL3038508] [UniProtKB: P0C1S7, P0C1U9] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
DNA gyrase subunit A/DNA gyrase subunit B/DNA gyrase in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094139] [GtoPdb: 3217, 3218] [UniProtKB: P0AES4, P0AES6]
ChEMBL	Inhibition of Escherichia coli DNA gyrase supercoiling incubated for 30 mins in presence of ATP	B	6.61	pIC50	244	nM	IC50	Eur J Med Chem (2023) 250: 115160-115160 [PMID:36753879]
ChEMBL	Inhibition of Escherichia coli DNA gyrase supercoiling activity	B	7.22	pIC50	60	nM	IC50	Bioorg Med Chem Lett (2022) 65: 128648-128648 [PMID:35231579]
DNA gyrase in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831]
ChEMBL	Inhibition of Staphylococcus aureus DNA gyrase assessed as reduction in DNA supercoiling using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorimetric assay	B	6.43	pIC50	374	nM	IC50	ACS Med Chem Lett (2021) 12: 1478-1485 [PMID:34527181]
ChEMBL	Inhibition of Staphylococcus aureus DNA gyrase supercoiling incubated for 30 mins in presence of ATP	B	6.43	pIC50	374	nM	IC50	Eur J Med Chem (2023) 250: 115160-115160 [PMID:36753879]
ChEMBL	Inhibition of Escherichia coli DNA gyrase assessed as reduction in DNA supercoiling using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorimetric assay	B	6.61	pIC50	244	nM	IC50	ACS Med Chem Lett (2021) 12: 1478-1485 [PMID:34527181]
ChEMBL	Inhibition of Staphylococcus aureus Gyrase supercoiling activity assessed as reduction in supercoiling pBR322 DNA by measuring relaxation by bromophenol blue staining based TAE gel method	B	6.77	pIC50	170	nM	IC50	J Med Chem (2021) 64: 15214-15249 [PMID:34614347]
ChEMBL	Inhibition of Staphylococcus aureus DNA gyrase	B	7.33	pIC50	47	nM	IC50	J Med Chem (2019) 62: 7445-7472 [PMID:31276392]
ChEMBL	Inhibition of Staphylococcus aureus DNA gyrase using positively supercoiled pBR322 DNA as substrate incubated for 25 mins by ethidium bromide staining based agarose gel electrophoresis method	B	7.33	pIC50	47	nM	IC50	J Med Chem (2020) 63: 5664-5674 [PMID:32027491]
DNA topoisomerase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
ChEMBL	Inhibition of human topoisomerase 2 assessed as reduction in decatenation	B	4.26	pIC50	55200	nM	IC50	Bioorg Med Chem Lett (2022) 65: 128648-128648 [PMID:35231579]
Topoisomerase IV in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038508] [UniProtKB: P0C1S7, P0C1U9]
ChEMBL	Inhibition of Staphylococcus aureus topoisomerase 4 assessed as reduction in decatenation using supercoiled pNO1 plasmid DNA as substrate incubated for 30 mins by fluorimetric assay	B	5.08	pIC50	8299	nM	IC50	ACS Med Chem Lett (2021) 12: 1478-1485 [PMID:34527181]
ChEMBL	Inhibition of Staphylococcus aureus DNA topoisomerase 4 relaxation activity measured for 30 mins	B	5.08	pIC50	8299	nM	IC50	Eur J Med Chem (2023) 250: 115160-115160 [PMID:36753879]
ChEMBL	Inhibition of Staphylococcus aureus topoisomerase IV decatenation activity using kDNA as substrate by ethidium bromide/bromophenol blue staining based agarose gel electrophoresis analysis	B	5.55	pIC50	2800	nM	IC50	J Med Chem (2021) 64: 15214-15249 [PMID:34614347]
ChEMBL	Inhibition of Staphylococcus aureus DNA topoisomerase 4	B	6.22	pIC50	600	nM	IC50	J Med Chem (2019) 62: 7445-7472 [PMID:31276392]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]