avibactam [Ligand Id: 10761] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1689063 (Avibactam, Nxl-104, NXL104, Nxl-104 free acid) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Bacterial beta-lactamase TEM in Bacteria (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364670] [UniProtKB: P62593] | ||||||||
| ChEMBL | Inhibition of bacterial Beta-lactamase TEM-1 (24 - 286) (unknown origin) expressed in Escherichia coli Transetta (DE3) | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2021) 41: 127956-127956 [PMID:33744439] |
| Beta-lactamase in Enterobacter cloacae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2725] [UniProtKB: P05364] | ||||||||
| ChEMBL | Inhibition of Enterobacter cloacae beta-lactamase P99 after 5 seconds incubation with nitrocefin substrate by spectrophotometry | B | 5.11 | pKi | 7700 | nM | Ki | Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316] |
| ChEMBL | Inhibition of Enterobacter cloacae AmpC | B | 6.03 | pIC50 | 923 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| ChEMBL | Inhibition of Enterobacter cloacae beta-lactamase P99 assessed as nitrocefin hydrolysis after 5 mins enzyme-compound preincubation | B | 7 | pIC50 | 100 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316] |
| Beta-lactamase in Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5031] [UniProtKB: P24735] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa beta-lactamase AmpC assessed as nitrocefin hydrolysis after 5 mins enzyme-compound preincubation | B | 6.89 | pIC50 | 128 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316] |
| Beta-lactamase 2 in Bacillus cereus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744488] [UniProtKB: P14488] | ||||||||
| ChEMBL | Inhibition of Bacillus cereus beta-lactamase II | B | 6.85 | pIC50 | 141.08 | nM | IC50 | Bioorg Med Chem Lett (2023) 88: 129308-129308 [PMID:37127102] |
| Beta-lactamase CTX-M-14 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287630] [UniProtKB: Q9L5C7] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-lactamase CTX-M-14 | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| Beta-lactamase OXA-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4951] [UniProtKB: P13661] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-lactamase OXA-1 | B | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| Beta-lactamase OXA-23 in Acinetobacter baumannii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3885669] [UniProtKB: Q9L4P2] | ||||||||
| ChEMBL | Inhibition of Acinetobacter baumannii OXA-23 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2020) 63: 7491-7507 [PMID:32150407] |
| ChEMBL | Inhibition of Acinetobacter baumannii beta-lactamase OXA-23 | B | 5.63 | pIC50 | 2320 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| Beta-lactamase TEM-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287599] [UniProtKB: Q4GY26] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-lactamase TEM-1 | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| BlaVIM-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255155] [UniProtKB: Q8GDC1] | ||||||||
| ChEMBL | Inhibition of recombinant Escherichia coli VIM-1 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | B | 4.4 | pKi | >40000 | nM | Ki | J Med Chem (2020) 63: 7491-7507 [PMID:32150407] |
| Carbepenem-hydrolyzing beta-lactamase KPC in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6132] [UniProtKB: Q9F663] | ||||||||
| ChEMBL | Inhibition of Klebsiella pneumoniae beta-lactamase KPC-2 | B | 6.73 | pIC50 | 186 | nM | IC50 | Eur J Med Chem (2022) 242: 114677-114677 [PMID:35988449] |
| Class A carbapenemase KPC-2 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5437] [UniProtKB: A8DS27] | ||||||||
| ChEMBL | Inhibition of recombinant Escherichia coli KPC-2 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition and measured every 10 secs for 10 mins by spectrophotometric analysis | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2020) 63: 7491-7507 [PMID:32150407] |
ChEMBL data shown on this page come from version 35:
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]
