sulbactam [Ligand Id: 10769] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL403 (CP-45899, CP-458992, NSC-759886, Sulbactam) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADC-14 protein in Acinetobacter genomosp. 3 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667675] [UniProtKB: Q0VTR6] | ||||||||
| ChEMBL | Inhibition of Acinetobacter genomosp. 3 isolate 65 ADC-14 | B | 5.95 | pIC50 | 1120 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1177-1184 [PMID:19029333] |
| ADC-16 protein in Acinetobacter genomosp. 3 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667676] [UniProtKB: Q0VTR8] | ||||||||
| ChEMBL | Inhibition of Acinetobacter genomosp. 3 isolate 103 ADC-16 | B | 5.11 | pIC50 | 7758 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1177-1184 [PMID:19029333] |
| ADC-18 protein in Acinetobacter genomosp. 3 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667677] [UniProtKB: Q0VTS0] | ||||||||
| ChEMBL | Inhibition of Acinetobacter genomosp. 3 isolate 195 ADC-18 | B | 4.93 | pIC50 | 11650 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1177-1184 [PMID:19029333] |
| Bacterial beta-lactamase TEM in Bacteria (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364670] [UniProtKB: P62593] | ||||||||
| ChEMBL | Cell Free Inhibition Assay: The inhibitory concentrations (IC50, [uM]) of the beta -lactamase inhibitors against purified TEM-1, SHV-1 and AmpC beta -lactamases are assessed by determining the concentration of inhibitor at which 50% of the nitrocefin hydrolysis is inhibited by the particular enzyme. Assays are performed with beta -lactamases expressed in the pET system (Novagen, San Diego, Calif.) without signal peptides. They contain an N-terminal hexa-Histidine tag that is used for purification on Ni-NTA (Qiagen, Hilden, Germany). The compounds are prepared as 50 mM stocks in DMSO and diluted into buffer P1 (50 mM phosphate, pH 7) to a final concentration of 10% DMSO. All further dilutions are done in P2 (P1 with 10% DMSO). Enzyme and compound dilutions are pre-incubated for 10 min at 37 C. and the reaction is started with the addition of pre-warmed (37 C.) nitrocefin at a final concentration of 50 mM. The change in absorption at 490 nm is followed at 37 C. for 10 min with 30 s intervals. | B | 5.97 | pIC50 | 1065.9 | nM | IC50 | US-9120808-B2. Substituted clavulanic acid (2015) |
| Beta-lactamase in Pseudomonas aeruginosa (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3885668] [UniProtKB: D2SSQ3] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa 531 beta-lactamase BEL-2 | B | 5.52 | pIC50 | 3000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 533-535 [PMID:19884378] |
| Beta-lactamase in Enterobacter cloacae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2725] [UniProtKB: P05364] | ||||||||
| ChEMBL | In vitro inhibitory activity against Beta-lactamase AmpC of class C enzyme | B | 4.18 | pIC50 | 66000 | nM | IC50 | J Med Chem (2003) 46: 2569-2571 [PMID:12801220] |
| ChEMBL | Inhibition of Enterobacter cloacae beta-lactamase P99 assessed as nitrocefin hydrolysis after 5 mins enzyme-compound preincubation | B | 4.68 | pIC50 | 21100 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316] |
| ChEMBL | In vitro inhibitory activity against Beta-lactamase TEM-1 of class A enzyme | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2003) 46: 2569-2571 [PMID:12801220] |
| ChEMBL | Compound was evaluated for beta-lactamase inhibition activity of Escherichia cloacae after 15 min of pre-incubation with the enzyme at 37 degree C | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2217-2222 |
| Beta-lactamase in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4114] [UniProtKB: P00807] | ||||||||
| ChEMBL | Inhibitory activity against Penicillinase from Staphylococcus aureus TH-14 using piperacillin (40 uM) as a substrate | B | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (1987) 30: 1469-1474 [PMID:3039137] |
| Beta-lactamase in Bacillus clausii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5439] [UniProtKB: A8RR46] | ||||||||
| ChEMBL | Inhibition of Bacillus clausii NR beta-lactamase BCL1 expressed in Escherichia coli BL21 (DE3) | B | 7.12 | pIC50 | 75 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 4009-4014 [PMID:17846134] |
| 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 | 4.57 | pIC50 | 27000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316] |
| Beta-lactamase 1 in Bacillus cereus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5732] [UniProtKB: P00809] | ||||||||
| ChEMBL | Inhibition of Beta-lactamase of Bacillus cereus (class A enzyme) without pre-incubation | B | 4.6 | pIC50 | 25000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2037-2040 |
| ChEMBL | Tested for the ability to inhibit Beta-lactamase of Bacillus cereus (class A enzyme) with 10 minutes pre-incubation | B | 4.6 | pIC50 | 25000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2037-2040 |
| Beta-lactamase AmpC in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2026] [UniProtKB: P00811] | ||||||||
| ChEMBL | In vitro inhibitory concentration against AmpC enzyme | B | 4.18 | pIC50 | 66000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 997-1000 [PMID:11327608] |
| ChEMBL | Inhibitory activity against AmpC (class C) beta-lactamase | B | 4.18 | pIC50 | 65900 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 991-996 [PMID:10230626] |
| ChEMBL | Inhibitory activity against AmpC (class C) beta-lactamase | B | 4.18 | pIC50 | 65900 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 997-1002 [PMID:10230627] |
| ChEMBL | Cell Free Inhibition Assay: The inhibitory concentrations (IC50, [uM]) of the beta -lactamase inhibitors against purified TEM-1, SHV-1 and AmpC beta -lactamases are assessed by determining the concentration of inhibitor at which 50% of the nitrocefin hydrolysis is inhibited by the particular enzyme. Assays are performed with beta -lactamases expressed in the pET system (Novagen, San Diego, Calif.) without signal peptides. They contain an N-terminal hexa-Histidine tag that is used for purification on Ni-NTA (Qiagen, Hilden, Germany). The compounds are prepared as 50 mM stocks in DMSO and diluted into buffer P1 (50 mM phosphate, pH 7) to a final concentration of 10% DMSO. All further dilutions are done in P2 (P1 with 10% DMSO). Enzyme and compound dilutions are pre-incubated for 10 min at 37 C. and the reaction is started with the addition of pre-warmed (37 C.) nitrocefin at a final concentration of 50 mM. The change in absorption at 490 nm is followed at 37 C. for 10 min with 30 s intervals. | B | 4.59 | pIC50 | 25495.4 | nM | IC50 | US-9120808-B2. Substituted clavulanic acid (2015) |
| Beta-lactamase bla(BEL1) in Pseudomonas aeruginosa (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3885670] [UniProtKB: Q3SAW3] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa 51170 beta-lactamase BEL-1 | B | 5.52 | pIC50 | 3000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 533-535 [PMID:19884378] |
| Beta-lactamase GES-13 in Pseudomonas aeruginosa (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250341] [UniProtKB: D1MIX9] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa GES-13 beta lactamase | B | 6.43 | pIC50 | 370 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1331-1333 [PMID:20065056] |
| Beta-lactamase OXA-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4951] [UniProtKB: P13661] | ||||||||
| ChEMBL | Inhibitory activity against Beta-lactamase type OXA1 (penicillinase) from Escherichia coli OXA1 using ampicillin (40 uM) as a substrate | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (1987) 30: 1469-1474 [PMID:3039137] |
| Beta-lactamase SCO-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075073] [UniProtKB: A1E3K9] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-lactamase SCO1 | B | 5.21 | pIC50 | 6200 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2185-2188 [PMID:17353248] |
| Beta-lactamase SHV-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5956] [UniProtKB: P0AD63] | ||||||||
| ChEMBL | Cell Free Inhibition Assay: The inhibitory concentrations (IC50, [uM]) of the beta -lactamase inhibitors against purified TEM-1, SHV-1 and AmpC beta -lactamases are assessed by determining the concentration of inhibitor at which 50% of the nitrocefin hydrolysis is inhibited by the particular enzyme. Assays are performed with beta -lactamases expressed in the pET system (Novagen, San Diego, Calif.) without signal peptides. They contain an N-terminal hexa-Histidine tag that is used for purification on Ni-NTA (Qiagen, Hilden, Germany). The compounds are prepared as 50 mM stocks in DMSO and diluted into buffer P1 (50 mM phosphate, pH 7) to a final concentration of 10% DMSO. All further dilutions are done in P2 (P1 with 10% DMSO). Enzyme and compound dilutions are pre-incubated for 10 min at 37 C. and the reaction is started with the addition of pre-warmed (37 C.) nitrocefin at a final concentration of 50 mM. The change in absorption at 490 nm is followed at 37 C. for 10 min with 30 s intervals. | B | 5.41 | pIC50 | 3915 | nM | IC50 | US-9120808-B2. Substituted clavulanic acid (2015) |
| Beta-lactamase SHV-11 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287606] [UniProtKB: Q7X575] | ||||||||
| ChEMBL | Inhibition of Escherichia coli JM109 beta-lactamase SHV-11 | B | 5.62 | pIC50 | 2400 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3792-3794 [PMID:18663019] |
| Beta-lactamase TEM in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2065] [UniProtKB: P62593] | ||||||||
| ChEMBL | Inhibition constant (Ki) for TEM-1 beta-lactamase | B | 6.1 | pKi | 800 | nM | Ki | J Med Chem (1988) 31: 370-374 [PMID:3257523] |
| ChEMBL | Inhibitory activity against Beta-lactamase from Bacillus sp. using penicillin G as substrate | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1987) 30: 1469-1474 [PMID:3039137] |
| ChEMBL | Inhibition of Escherichia coli K12 TEM1 | B | 5.14 | pIC50 | 7300 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2185-2188 [PMID:17353248] |
| ChEMBL | Inhibitory activity against TEM-1 (class A) beta-lactamase | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 991-996 [PMID:10230626] |
| ChEMBL | Inhibitory activity against TEM-1 (class A) beta-lactamase | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 997-1002 [PMID:10230627] |
| ChEMBL | In vitro inhibitory concentration against TEM-1 enzyme | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 997-1000 [PMID:11327608] |
| ChEMBL | Compound was evaluated for beta-lactamase inhibition activity of Escherichia coli after 15 min of pre-incubation with the enzyme at 37 degree C | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2217-2222 |
| Beta-lactamase type II in Bacteroides fragilis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4840] [UniProtKB: P25910] | ||||||||
| ChEMBL | In vitro inhibitory concentration against CCRA enzyme | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 997-1000 [PMID:11327608] |
| Carbapenem-hydrolizing beta-lactamase SFC-1 in Serratia fonticola (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5042] [UniProtKB: Q6JP75] | ||||||||
| ChEMBL | Inhibition of Serratia fonticola UTAD54 SFC1 beta lactamase expressed in Escherichia coli BL21(DE3) by SDS-PAGE | B | 4.64 | pIC50 | 22700 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 4512-4514 [PMID:17875998] |
| Class D beta-lactamase in Brachyspira pilosicoli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255145] [UniProtKB: Q50H31] | ||||||||
| ChEMBL | Inhibition of Brachyspira pilosicoli beta-lactamase OXA-63 expressed in Escherichia coli BL21 (DE3) assessed as reduction in nitrocefin hydrolysis by spectrophotometry relative to oxacillin | B | 4.92 | pIC50 | 12000 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1264-1268 [PMID:18212108] |
| Extended-spectrum beta-lactamase PER-6 in Aeromonas allosaccharophila (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697666] [UniProtKB: D5HSX5] | ||||||||
| ChEMBL | Inhibition of Aeromonas allosaccharophila AL-1 beta-lactamase PER6 | B | 5.4 | pIC50 | 4000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1619-1622 [PMID:20145085] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of recombinant SARS-CoV-2 Main protease using ALNDFSNSGSDVLYQPPQTSITSAVLQ/SGFRKMAFPS-NH2 as substrate preincubated for 45 to 75 mins followed by substrate addition measured after 6 mins by SPE-MS inhibition assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 7682-7696 [PMID:35549342] |
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]
