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ChEMBL ligand: CHEMBL2158050 |
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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 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 by fluorescence based microtiter plate reader assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | Bioorg Med Chem Lett (2022) 57: 128499-128499 [PMID:34906671] |
DNA gyrase in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831] | ||||||||
ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase | B | 5.81 | pIC50 | 1560 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2955-2961 [PMID:23566517] |
ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase supercoiling activity using pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence based microtiter plate reader assay | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (2022) 57: 128499-128499 [PMID:34906671] |
ChEMBL | Inhibition of wild type Staphylococcus aureus DNA gyrase subunit 2GyrA/2GyrB assessed as pBR322 supercoiling after 1 hr | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2013) 56: 7396-7415 [PMID:23968485] |
DNA gyrase subunit A in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424506] [UniProtKB: P20831] | ||||||||
ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase A assessed as reduction in enzyme-mediated supercoiling of relaxed pBR322 DNA measured after 60 mins by electrophoresis method | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2019) 62: 7445-7472 [PMID:31276392] |
ChEMBL | Inhibition of quinolone-resistant Staphylococcus aureus A-798 DNA gyrase S84L mutant assessed as pBR322 supercoiling after 1 hr | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2013) 56: 7396-7415 [PMID:23968485] |
DNA gyrase subunit A in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1858] [GtoPdb: 3217] [UniProtKB: P0AES4] | ||||||||
ChEMBL | Inhibition of Escherichia coli DNA gyrase A assessed as reduction in enzyme-mediated supercoiling of relaxed pBR322 DNA measured after 60 mins by electrophoresis method | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2019) 62: 7445-7472 [PMID:31276392] |
ChEMBL | Inhibition of Escherichia coli N-terminal His6-tagged DNA gyrase A expressed in Escherichia coli using relaxed pBR322 DNA as substrate incubated for 1 hr by agarose gel electrophoresis method | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2020) 63: 5664-5674 [PMID:32027491] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG channel in HEK293 cells by voltage-gated patch clamp technique | B | 4.63 | pIC50 | 23600 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2955-2961 [PMID:23566517] |
ChEMBL | Inhibition of human ERG | B | 4.63 | pIC50 | 23600 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3353-3358 [PMID:28610977] |
Topoisomerase IV in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038508] [UniProtKB: P0C1S7, P0C1U9] | ||||||||
ChEMBL | Inhibition of Staphylococcus aureus topoisomerase 4 using pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence based microtiter plate reader assay | B | 5.06 | pIC50 | 8800 | nM | IC50 | Bioorg Med Chem Lett (2022) 57: 128499-128499 [PMID:34906671] |
ChEMBL | Inhibition of Staphylococcus aureus RN4220 DNA topoisomerase 4 expressed in Escherichia coli BL21(DE3) cells using supercoiled pBR322 DNA as substrate by agarose gel electrophoresis method | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2020) 63: 5664-5674 [PMID:32027491] |
Topoisomerase IV subunit A in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4088] [UniProtKB: P0C1U9] | ||||||||
ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 subunit ParC assessed as reduction in decatenation of kinetoplast DNA incubated for 60 mins by ethidium bromide staining based gel electrophoresis method | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2019) 62: 7445-7472 [PMID:31276392] |
DNA topoisomerase 4 subunit A/Topoisomerase IV subunit A in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1895] [GtoPdb: 3225] [UniProtKB: P0AFI2] | ||||||||
ChEMBL | Inhibition of Escherichia coli DNA topoisomerase 4 subunit ParC assessed as reduction in decatenation of kinetoplast DNA incubated for 60 mins by ethidium bromide staining based gel electrophoresis method | B | 5.66 | pIC50 | 2200 | 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]