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ChEMBL ligand: CHEMBL3317856 (Gepotidacin, GSK-2140944, GSK2140944) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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] |
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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]