zoliflodacin [Ligand Id: 10875] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3544978 (AZD-0914, AZD0914, ETX-0914, ETX0914, Zoliflodacin, Zoliflodacina, Zoliflodacine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DNA gyrase in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aureus ATTC 25923 DNA gyrase | B | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2022) 65: 6903-6925 [PMID:35500229] |
| DNA gyrase subunit A in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1858] [GtoPdb: 3217] [UniProtKB: P0AES4] | ||||||||
| ChEMBL | Fluorescence Polarisation Assay: In a black, 384-well polystyrene assay plate, 30 microliters/well of 5 nM Escherichia coli DNA gyrase A/B tetramer and 130 micrograms/mL of topological^ relaxed plasmid containing the triplex-forming sequence TTCTTCTTCTTCTTCTTCTTCTTCTTC (SEQ ID NO: 1) in an assay buffer consisting of 35 mM Tris-HCI (pH 7.5), 24 mM KCI, 4 mM MgCI2, 2 mM dithiothreitol, 1.8 mM spermidine, 5% (v/v) glycerol, 200 nM bovine serum albumin, 0.8%dimethylsulfoxide, and 0.3 mM ATP were incubated at ambient temperature for (typically 30 minutes) in the absence or presence of 5 -10 different concentrations of test compound. The supercoiling reactions were quenched by the addition of 10 microliters/well of 40 nM oligodeoxynucleotide probe in 3X triplex-forming buffer consisting of 150 mM NaCI, and 150 mM sodium acetate at pH 3.5. The oligodeoxynucleotide probe was 5'-BODIPY-FL-labeled TTCTTCTTC (SEQ ID NO:2). After 60 minutes, the fluorescence anisotropy of the BODIPY- FL was measured in a Tecan Ultra plate. | B | 6.77 | pIC50 | 169 | nM | IC50 | US-8889671-B2. Compounds and methods for treating bacterial infections (2014) |
| DNA gyrase subunit A/DNA gyrase subunit B in Mycobacterium tuberculosis (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430898] [UniProtKB: P9WG45, P9WG47] | ||||||||
| ChEMBL | Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase | B | 4.49 | pIC50 | 32000 | nM | IC50 | J Med Chem (2022) 65: 6903-6925 [PMID:35500229] |
| DNA gyrase in Escherichia coli [GtoPdb: 3219] | ||||||||
| GtoPdb | DNA gyrase supercoiling assay | - | 6.77 | pIC50 | 169 | nM | IC50 | US8889671B2. Compounds and methods for treating bacterial infections (2014) |
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]
