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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 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 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 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 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]