novobiocin [Ligand Id: 12021] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL36506 (Albamycin, Albamycin t, Cathomycin, Novobiocin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining | B | 4.07 | pIC50 | 85100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 180-183 [PMID:19932960] |
| ChEMBL | Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay | B | 4.18 | pIC50 | 66069.34 | nM | IC50 | Bioorg Med Chem (2008) 16: 8224-8236 [PMID:18678495] |
| ChEMBL | TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells | F | 4.6 | pIC50 | 25000 | nM | IC50 | Placenta (2006) 27: 1096-1102 [PMID:16460798] |
| 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 ATPase activity using DNA as substrate after 60 mins | B | 6.61 | pIC50 | 245 | nM | IC50 | Medchemcomm (2017) 8: 942-951 [PMID:30034678] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase using relaxed pNO1 plasmid and biotinylated oligonucelotide incubated for 30 mins by fluorescence based DNA super-coiling assay | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase assessed as reduction in relaxation of supercoiled pNO1 DNA measured after 30 mins by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2021) 213: 113200-113200 [PMID:33524686] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Medchemcomm (2019) 10: 1007-1017 [PMID:31303999] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase using biotinylated oligonucleotide as substrate incubated for 30 mins in presence of ATP by fluorescence-based microplate reader assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2019) 167: 269-290 [PMID:30776691] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 6.77 | pIC50 | 168 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2433-2440 [PMID:33329764] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase assessed as inhibition of pUC19 supercoiling after 30 mins by agarose gel electrophoresis | B | 6.84 | pIC50 | 144 | nM | IC50 | Medchemcomm (2017) 8: 942-951 [PMID:30034678] |
| ChEMBL | Inhibition of reconstituted Escherichia coli DNA gyrase subunit AB assessed as reduction of DNA supercoiling activity using pBR322 DNA substrate | B | 7 | pIC50 | 100 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1382-1390 [PMID:18268084] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase using relaxed pBR322 DNA as substrate after 3 hrs by DNA super-coiling assay | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
| GtoPdb | DNA gyrase supercoiling assay | - | 7.1 | pIC50 | 80 | nM | IC50 | J Antimicrob Chemother (2011) 66: 2061-9 [PMID:21693461] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase by measuring supercoiling activity incubated for 60 mins by fluorescence based assay | B | 7.62 | pIC50 | 23.88 | nM | IC50 | Bioorg Med Chem (2020) 28: 115776-115776 [PMID:33032189] |
| DNA gyrase in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2008) 51: 5243-5263 [PMID:18690678] |
| ChEMBL | Inhibition of Staphylococcus aureus N-terminal His6-tagged DNA gyrase subunit GyrA/GyrB supercoiling activity expressed in Escherichia coli BL21 (DE3) using relaxed pBR322 DNA as substrate after 1 hr by agarose gel electrophoresis | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2017) 60: 3755-3775 [PMID:28406299] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2433-2440 [PMID:33329764] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase using biotinylated oligonucleotide as substrate incubated for 30 mins in presence of ATP by fluorescence-based microplate reader assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2019) 167: 269-290 [PMID:30776691] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase assessed as supercoiling of relaxed pNO1 plasmid after 30 mins by SybrGOLD staining based fluorescence assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2016) 117: 197-211 [PMID:27100032] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Medchemcomm (2019) 10: 1007-1017 [PMID:31303999] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase A/DNA gyrase B supercoiling activity using relaxed pNO1 DNA as substrate after 30 mins in presence of biotin-labeled oligonucleotide by SybrGOLD staining based fluorescence assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2017) 130: 171-184 [PMID:28246042] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase supercoiling activity using relaxed pHOT-1 DNA as substrate after 60 mins by ethidium bromide-based gel electrophoresis | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2019) 62: 2950-2973 [PMID:30698430] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase using relaxed pNO1 plasmid and biotinylated oligonucelotide incubated for 30 mins by fluorescence based DNA super-coiling assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase assessed reduction in relaxation of supercoiled pNO1 DNA measured after 30 mins by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2021) 213: 113200-113200 [PMID:33524686] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase-mediated supercoiling of relaxed DNA using pBR 322 as substrate by agarose gel electrophoresis analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2014) 22: 5970-5987 [PMID:25288496] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase assessed as supercoiling of relaxed pBR322 plasmid after 45 mins by ethidium bromide staining based agarose gel electrophoresis | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2016) 117: 197-211 [PMID:27100032] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase using relaxed pBR322 DNA as substrate after 3 hrs by DNA super-coiling assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase | B | 8.4 | pIC50 | <4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7127-7130 [PMID:23084277] |
| DNA gyrase subunit A/DNA gyrase subunit B in Escherichia coli [GtoPdb: 3217, 3218] [UniProtKB: P0AES4, P0AES6] | ||||||||
| GtoPdb | DNA gyrase supercoiling assay | - | 7.1 | pIC50 | 80 | nM | IC50 | J Antimicrob Chemother (2011) 66: 2061-9 [PMID:21693461] |
| 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 DNA gyrase assessed as inhibition of supercoiling activity using relaxed pBR322 plasmid as substrate after 30 mins | B | 4.34 | pIC50 | 46000 | nM | IC50 | Bioorg Med Chem (2016) 24: 42-52 [PMID:26678175] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase activity | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2998-3003 [PMID:30122228] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase super coiling activity of relaxed pBR322 using ethidium bromide staining by agarose gel electrophoresis | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2013) 70: 143-153 [PMID:24148991] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase using relaxed pBR322 as substrate after 30 mins by supercoiling assay | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem (2014) 22: 6552-6563 [PMID:25456076] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining and electrophoresis based DNA supercoiling assay | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem (2015) 23: 2062-2078 [PMID:25801151] |
| ChEMBL | Inhibition of DNA gyrase GyrA/GyrB in Mycobacterium tuberculosis incubated for 30 mins assessed as reduction in supercoiling of relaxed relaxed pBR322 DNA by ethidium bromide staining based agarose gel electrophoresis method | B | 7.34 | pIC50 | 46 | nM | IC50 | Eur J Med Chem (2015) 103: 1-16 [PMID:26318054] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling activity using relaxed pBR322 as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis | B | 7.34 | pIC50 | 46 | nM | IC50 | Eur J Med Chem (2016) 124: 160-185 [PMID:27569197] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase supercoiling activity using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining method | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem (2014) 22: 4924-4934 [PMID:25129171] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem (2016) 24: 877-885 [PMID:26787274] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase ATPase activity | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2998-3003 [PMID:30122228] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase-mediated relaxed pBR322 DNA supercoiling by gel electrophoresis | B | 7.82 | pIC50 | 15 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1005-1009 [PMID:25221657] |
| DNA gyrase subunit B in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1826] [GtoPdb: 3218] [UniProtKB: P0AES6] | ||||||||
| ChEMBL | Binding affinity to Escherichia coli GyrB | B | 7.55 | pKd | 28 | nM | Kd | J Med Chem (2011) 54: 915-929 [PMID:21235241] |
| ChEMBL | Binding affinity to Escherichia coli H560 DNA gyrase B | B | 8.15 | pKd | 7 | nM | Kd | Eur J Med Chem (2016) 124: 160-185 [PMID:27569197] |
| ChEMBL | Inhibition of Escherichia coli H560 DNA gyrase B ATPase activity after 30 mins by ammonium molybdate/malachite green-based phosphate detection assay | B | 8.15 | pKi | 7 | nM | Ki | Eur J Med Chem (2016) 124: 160-185 [PMID:27569197] |
| ChEMBL | Inhibition of Escherichia coli JM109 DNA gyrase subunit B assessed as DNA triple helix formation by supercoiling assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1982-1990 [PMID:18347114] |
| ChEMBL | Inhibition of Escherichia coli DNA gyrase B ATP binding site assessed as reduction in supercoiling of relaxed pNO1 DNA after 30 mins in presence of biotinylated oligonucleotide by sybrGOLD staining based fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2016) 59: 8941-8954 [PMID:27541007] |
| ChEMBL | Inhibition of Escherichia coli ATCC 25922 DNA gyrase B using relaxed pNO1 DNA as substrate incubated for 30 mins and measured by sybrGOLD staining based fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2017) 125: 500-514 [PMID:27689732] |
| ChEMBL | Inhibition of Escherichia coli C-terminal His6-tagged DNA gyrase B expressed in Escherichia coli BL21(DE3) preincubated for 10 mins followed by ATP addition measured after 30 mins by purine nucleoside phosphorylase enzyme coupled spectrophotometric method | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2018) 154: 117-132 [PMID:29778894] |
| ChEMBL | Inhibition of Escherichia coli JM109 DNA gyrase subunit B assessed as ATP hydrolysis by ATPase assay | B | 6.81 | pIC50 | 154 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1982-1990 [PMID:18347114] |
| GtoPdb | DNA gyrase supercoiling assay | - | 7.1 | pIC50 | 80 | nM | IC50 | J Antimicrob Chemother (2011) 66: 2061-9 [PMID:21693461] |
| DNA gyrase subunit B in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921666] [UniProtKB: P0A0K8] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase B ATPase activity | B | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg Med Chem (2014) 22: 5970-5987 [PMID:25288496] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase B using relaxed pNO1 DNA as substrate incubated for 30 mins and measured by sybrGOLD staining based fluorescence assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2017) 125: 500-514 [PMID:27689732] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase B preincubated for 10 mins followed by ATP addition measured after 30 mins by purine nucleoside phosphorylase enzyme coupled spectrophotometric method | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2018) 154: 117-132 [PMID:29778894] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase B ATP binding site assessed as reduction in supercoiling of relaxed pNO1 DNA after 30 mins in presence of biotinylated oligonucleotide by sybrGOLD staining based fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2016) 59: 8941-8954 [PMID:27541007] |
| DNA gyrase subunit B in Mycobacterium smegmatis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085613] [UniProtKB: P0C559] | ||||||||
| ChEMBL | Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) after 2 hrs | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2013) 70: 143-153 [PMID:24148991] |
| ChEMBL | Inhibition of purified Mycobacterium smegmatis GyrB at 50 to 100 uM after 100 mins by ATPase assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2014) 22: 6552-6563 [PMID:25456076] |
| ChEMBL | Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2014) 22: 4924-4934 [PMID:25129171] |
| ChEMBL | Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2015) 23: 2062-2078 [PMID:25801151] |
| ChEMBL | Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2015) 103: 1-16 [PMID:26318054] |
| ChEMBL | Inhibition of Mycobacterium smegmatis DNA GyrB domain assessed as inhibition of inorganic phosphate release after 100 mins at room temperature by ATPase assay | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem (2015) 23: 1402-1412 [PMID:25766629] |
| DNA gyrase subunit B in Escherichia coli [GtoPdb: 3218] [UniProtKB: P0AES6] | ||||||||
| GtoPdb | DNA gyrase supercoiling assay | - | 7.1 | pIC50 | 80 | nM | IC50 | J Antimicrob Chemother (2011) 66: 2061-9 [PMID:21693461] |
| DNA gyrase subunit B in Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075021] [UniProtKB: P0A4L9] | ||||||||
| ChEMBL | Inhibition of Streptococcus pneumoniae SP-3 gyrB by enzyme coupled phosphate assay | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5302-5306 [PMID:19683922] |
| DNA gyrase subunit B in Mycobacterium smegmatis (strain ATCC 700084 / mc(2)155) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6059] [UniProtKB: A0QNE0] | ||||||||
| ChEMBL | Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based assay | B | 7.34 | pIC50 | 46 | nM | IC50 | Eur J Med Chem (2016) 122: 216-231 [PMID:27371925] |
| DNA topoisomerase 4 subunit B in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150841] [UniProtKB: P0C1S7] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aures ParE using pBR322 DNA as substrate in presence of ATP | B | 5.1 | pIC50 | 7900 | nM | IC50 | Eur J Med Chem (2020) 188: 112022-112022 [PMID:31901744] |
| Genome polyprotein in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523954] [UniProtKB: A0A024AXB9] | ||||||||
| ChEMBL | Inhibition of Zika virus NS2B-NS3 protease | B | 4.85 | pIC50 | 14200 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339] |
| ChEMBL | Inhibition of Zika virus NS2B-NS3 protease by cell based assay | B | 4.61 | pEC50 | 24800 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339] |
| Microtubule-associated proteins 1A/1B light chain 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879518] [UniProtKB: Q9H492] | ||||||||
| ChEMBL | Binding affinity to human LC3A expressed in Escherichia coli BL21-(DE3) by isothermal titration calorimetry | B | 5.12 | pKd | 7500 | nM | Kd | J Med Chem (2021) 64: 3720-3746 [PMID:33769048] |
| ChEMBL | Displacement of sGFP-p62-LIR peptide from human N-terminal SNAP-fused LC3A by time-resolved FRET assay | B | 5.06 | pKi | 8800 | nM | Ki | J Med Chem (2021) 64: 3720-3746 [PMID:33769048] |
| ChEMBL | Displacement of sGFP-p62-LIR peptide from human N-terminal SNAP-fused LC3A by time-resolved FRET assay | B | 4.37 | pIC50 | 42900 | nM | IC50 | J Med Chem (2021) 64: 3720-3746 [PMID:33769048] |
| Microtubule-associated proteins 1A/1B light chain 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879514] [UniProtKB: Q9GZQ8] | ||||||||
| ChEMBL | Binding affinity to human LC3B expressed in Escherichia coli BL21-(DE3) by isothermal titration calorimetry | B | 4.76 | pKd | 17400 | nM | Kd | J Med Chem (2021) 64: 3720-3746 [PMID:33769048] |
| ChEMBL | Displacement of sGFP-p62-LIR peptide from human N-terminal SNAP-fused LC3B by time-resolved FRET assay | B | 4.71 | pKi | 19300 | nM | Ki | J Med Chem (2021) 64: 3720-3746 [PMID:33769048] |
| ParE in Streptococcus pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075022] [UniProtKB: Q7X1P7] | ||||||||
| ChEMBL | Inhibition of Streptococcus pneumoniae SP-3 parE after 30 mins | B | 5.69 | pIC50 | 2030 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5302-5306 [PMID:19683922] |
| Topoisomerase IV in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038508] [UniProtKB: P0C1S7, P0C1U9] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 using relaxed pNO1 plasmid and biotinylated oligonucelotide incubated for 30 mins by fluorescence based DNA relaxation assay | B | 4.57 | pIC50 | 27000 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 using supercoiled pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 4.57 | pIC50 | 27000 | nM | IC50 | Medchemcomm (2019) 10: 1007-1017 [PMID:31303999] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 using biotinylated oligonucleotide as substrate incubated for 30 mins in presence of ATP by fluorescence-based microplate reader assay | B | 4.57 | pIC50 | 27000 | nM | IC50 | Eur J Med Chem (2019) 167: 269-290 [PMID:30776691] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 using supercoiled pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence assay | B | 4.57 | pIC50 | 27000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2433-2440 [PMID:33329764] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA topoisomerase 4 using kinetoplast DNA as substrate by decatenation assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2015) 58: 5501-5521 [PMID:26098163] |
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]
