ChEMBL ligand: CHEMBL777 (BRL 14151, BRL-14151, Clavulanate, Clavulanic acid, Clavulanic Acid, RX-10100, Serdaxin)
Bacterial beta-lactamase TEM in Bacteria [ChEMBL: CHEMBL2364670] [UniProtKB: P62593] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase in Pseudomonas aeruginosa [ChEMBL: CHEMBL3885668] [UniProtKB: D2SSQ3] Beta-lactamase in Enterobacter cloacae [ChEMBL: CHEMBL2725] [UniProtKB: P05364] Beta-lactamase in S.aureus [ChEMBL: CHEMBL4114] [UniProtKB: P00807] Beta-lactamase in Pseudomonas luteola [ChEMBL: CHEMBL3308938] [UniProtKB: Q670S6] Beta-lactamase in Bacillus clausii [ChEMBL: CHEMBL5439] [UniProtKB: A8RR46] Beta-lactamase in Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228) [ChEMBL: CHEMBL5031] [UniProtKB: P24735] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase AmpC in Escherichia coli [ChEMBL: CHEMBL2026] [UniProtKB: P00811] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase bla(BEL1) in Pseudomonas aeruginosa [ChEMBL: CHEMBL3885670] [UniProtKB: Q3SAW3] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase class C in Enterobacter cloacae [ChEMBL: CHEMBL3499] [UniProtKB: Q59401] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase CTX-M in Escherichia coli [ChEMBL: CHEMBL6131] [UniProtKB: Q9EXV5] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase GES-13 in Pseudomonas aeruginosa [ChEMBL: CHEMBL1250341] [UniProtKB: D1MIX9] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase OXA-1 in Escherichia coli [ChEMBL: CHEMBL4951] [UniProtKB: P13661] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase SCO-1 in Escherichia coli [ChEMBL: CHEMBL1075073] [UniProtKB: A1E3K9] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase SHV-1 in Escherichia coli [ChEMBL: CHEMBL5956] [UniProtKB: P0AD63] Beta-lactamase SHV-1 in Klebsiella pneumoniae [ChEMBL: CHEMBL5094] [UniProtKB: P0AD64] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase SHV-5 in Klebsiella pneumoniae [ChEMBL: CHEMBL1075174] [UniProtKB: P0A3M1] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase SHV-55 in Klebsiella pneumoniae [ChEMBL: CHEMBL1255144] [UniProtKB: Q4TVR4] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase SHV-72 in Klebsiella pneumoniae [ChEMBL: CHEMBL1255121] [UniProtKB: A0ZX81] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase TEM in Escherichia coli [ChEMBL: CHEMBL2065] [UniProtKB: P62593] There should be some charts here, you may need to enable JavaScript!
Beta-lactamase TEM-125 in Escherichia coli [ChEMBL: CHEMBL5041] [UniProtKB: Q6GWS8] There should be some charts here, you may need to enable JavaScript!
Carbapenem-hydrolizing beta-lactamase SFC-1 in Serratia fonticola [ChEMBL: CHEMBL5042] [UniProtKB: Q6JP75] There should be some charts here, you may need to enable JavaScript!
Carbepenem-hydrolyzing beta-lactamase KPC in Klebsiella pneumoniae [ChEMBL: CHEMBL6132] [UniProtKB: Q9F663] There should be some charts here, you may need to enable JavaScript!
Class D beta-lactamase in Brachyspira pilosicoli [ChEMBL: CHEMBL1255145] [UniProtKB: Q50H31] There should be some charts here, you may need to enable JavaScript!
Extended-spectrum beta-lactamase CTX-M-53 in Salmonella enterica subsp. enterica serovar Westhampton [ChEMBL: CHEMBL1667678] [UniProtKB: Q2XPY6] There should be some charts here, you may need to enable JavaScript!
Gil1 in Citrobacter gillenii [ChEMBL: CHEMBL1075063] [UniProtKB: A4KCT8] There should be some charts here, you may need to enable JavaScript!
elastase, neutrophil expressed/Leukocyte elastase in Human [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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	7.53	pIC50	29.5	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	7	pIC50	100	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	Compound was evaluated for beta-lactamase inhibition activity of Enterobacter cloacae after 15 min of pre-incubation with the enzyme at 37 degree C	B	4	pIC50	100000	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2217-2222
ChEMBL	Inhibition of Enterobacter cloacae beta-lactamase P99 assessed as nitrocefin hydrolysis after 5 mins enzyme-compound preincubation	B	4	pIC50	>100000	nM	IC50	Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316]
ChEMBL	Inhibitory activity against beta-Lactamase enzyme derived from Enterobacter cloacae P99	B	4.7	pIC50	>20000	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1513-1518
ChEMBL	Inhibitory activity against beta-Lactamase enzyme derived from Enterobacter cloacae SC 12368 E-2	B	4.7	pIC50	>20000	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1513-1518
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	7.1	pIC50	80	nM	IC50	J Med Chem (1987) 30: 1469-1474 [PMID:3039137]
Beta-lactamase in Pseudomonas luteola (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308938] [UniProtKB: Q670S6]
ChEMBL	Inhibition of Pseudomonas luteola LAM Beta-lactamase LUT-1	B	7.44	pIC50	36	nM	IC50	Antimicrob Agents Chemother (2010) 54: 45-51 [PMID:19884377]
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	7.07	pIC50	85	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	pIC50	>100000	nM	IC50	Antimicrob Agents Chemother (2010) 54: 5132-5138 [PMID:20921316]
ChEMBL	Inhibitory concentration was evaluated as concentration required for 50% inhibition of Pseudomonas aeruginosa 18SH Beta-lactamase	B	6.1	pIC50	800	nM	IC50	J Med Chem (1998) 41: 3961-3971 [PMID:9767633]
Beta-lactamase AmpC in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2026] [UniProtKB: P00811]
ChEMBL	Inhibitory activity against Escherichia coli TEM-3 Beta-lactamase	B	7.82	pIC50	15	nM	IC50	J Med Chem (1998) 41: 3961-3971 [PMID:9767633]
ChEMBL	Inhibitory activity against Escherichia coli TEM-3 Beta-lactamase	B	7.82	pIC50	15	nM	IC50	J Med Chem (1998) 41: 3961-3971 [PMID:9767633]
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	7	pIC50	100	nM	IC50	Antimicrob Agents Chemother (2010) 54: 533-535 [PMID:19884378]
Beta-lactamase class C in Enterobacter cloacae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3499] [UniProtKB: Q59401]
ChEMBL	The compound was tested for its inhibitory activity towards Class C beta-lactamase from Enterobacter cloacae 908R at 0.8 umol concentration	B	4	pIC50	100000	nM	IC50	Bioorg Med Chem Lett (2002) 12: 971-975 [PMID:11959006]
Beta-lactamase CTX-M in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6131] [UniProtKB: Q9EXV5]
ChEMBL	Inhibition of Escherichia coli CTX-M-15	B	8.05	pIC50	9	nM	IC50	Antimicrob Agents Chemother (2007) 51: 3089-3095 [PMID:17591851]
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	7	pIC50	100	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	5.49	pIC50	3200	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	7.15	pIC50	70	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	7.52	pIC50	30.3	nM	IC50	US-9120808-B2. Substituted clavulanic acid (2015)
ChEMBL	Inhibition of Escherichia coli SHV1	B	7.55	pIC50	28	nM	IC50	J Med Chem (2007) 50: 4113-4121 [PMID:17665896]
Beta-lactamase SHV-1 in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5094] [UniProtKB: P0AD64]
ChEMBL	Inhibition of Klebsiella pneumoniae Beta-Lactamase SHV-1	B	6.77	pIC50	170	nM	IC50	Antimicrob Agents Chemother (2008) 52: 1806-1811 [PMID:18316518]
ChEMBL	Inhibition of Klebsiella pneumoniae Beta-Lactamase SHV-1	B	6.77	pIC50	170	nM	IC50	Antimicrob Agents Chemother (2008) 52: 1897-1898 [PMID:18316524]
Beta-lactamase SHV-5 in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075174] [UniProtKB: P0A3M1]
ChEMBL	Inhibition of Klebsiella pneumoniae beta-lactamase SHV-105	B	4.6	pKi	25360	nM	Ki	Med Chem Res (2012) 21: 2229-2237
Beta-lactamase SHV-55 in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255144] [UniProtKB: Q4TVR4]
ChEMBL	Inhibition of Klebsiella pneumoniae Beta-Lactamase SHV-55	B	7.7	pIC50	20	nM	IC50	Antimicrob Agents Chemother (2008) 52: 1897-1898 [PMID:18316524]
Beta-lactamase SHV-72 in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255121] [UniProtKB: A0ZX81]
ChEMBL	Inhibition of Klebsiella pneumoniae Beta-Lactamase SHV-72	B	5.76	pIC50	1720	nM	IC50	Antimicrob Agents Chemother (2008) 52: 1806-1811 [PMID:18316518]
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	The compound was tested for its inhibitory activity towards Class A TEM-1 beta-lactamase from Escherichia coli at 0.3 umol	B	4.6	pIC50	25000	nM	IC50	Bioorg Med Chem Lett (2002) 12: 971-975 [PMID:11959006]
ChEMBL	Inhibitory activity against Beta-lactamase type TEM2 (penicillinase) from Escherichia coli TEM2 using penicillin G (40 uM) as a substrate	B	4.68	pIC50	21000	nM	IC50	J Med Chem (1987) 30: 1469-1474 [PMID:3039137]
ChEMBL	Inhibition of Escherichia coli K12 TEM1	B	6.77	pIC50	170	nM	IC50	Antimicrob Agents Chemother (2007) 51: 2185-2188 [PMID:17353248]
ChEMBL	Inhibition of Escherichia coli DH5alpha beta-lactamase TEM-1	B	7.1	pIC50	80	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4181-4183 [PMID:17709463]
ChEMBL	Inhibitory activity against beta-Lactamase enzyme derived from Escherichia coli WC3310 TEM-2	B	7.22	pIC50	60	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1513-1518
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	7.4	pIC50	40	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2217-2222
ChEMBL	Inhibition of Escherichia coli TEM1	B	7.52	pIC50	30	nM	IC50	J Med Chem (2007) 50: 4113-4121 [PMID:17665896]
Beta-lactamase TEM-125 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5041] [UniProtKB: Q6GWS8]
ChEMBL	Inhibition of Escherichia coli DH5alpha beta-lactamase TEM-158	B	5.07	pIC50	8600	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4181-4183 [PMID:17709463]
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	4.14	pIC50	72800	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4512-4514 [PMID:17875998]
Carbepenem-hydrolyzing beta-lactamase KPC in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6132] [UniProtKB: Q9F663]
ChEMBL	Inhibition of Klebsiella pneumoniae 1534 beta-lactamase KPC-2 by competitive assay	B	4.96	pKi	11000	nM	Ki	Antimicrob Agents Chemother (2010) 54: 2867-2877 [PMID:20421396]
ChEMBL	Inhibition of carbapenem-resistant Klebsiella pneumoniae carbepenem-hydrolyzing beta-lactamase KPC-1	B	4.98	pIC50	10500	nM	IC50	Antimicrob Agents Chemother (2010) 54: 328-332 [PMID:19901091]
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	5.7	pIC50	2000	nM	IC50	Antimicrob Agents Chemother (2008) 52: 1264-1268 [PMID:18212108]
Extended-spectrum beta-lactamase CTX-M-53 in Salmonella enterica subsp. enterica serovar Westhampton (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667678] [UniProtKB: Q2XPY6]
ChEMBL	Inhibition of Salmonella enterica serotype Westhampton beta-lactamase CTX-M-53	B	8	pIC50	10	nM	IC50	Antimicrob Agents Chemother (2009) 53: 1944-1951 [PMID:19273683]
Gil1 in Citrobacter gillenii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075063] [UniProtKB: A4KCT8]
ChEMBL	Inhibition of Citrobacter gillenii CIP 106783 Beta-lactamase GIL1 expressed in Escherichia coli DH10B	B	8.05	pIC50	9	nM	IC50	Antimicrob Agents Chemother (2007) 51: 1365-1372 [PMID:17242148]
elastase, neutrophil expressed/Leukocyte elastase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
ChEMBL	Inhibitory concentration which is required to cause 50% inhibition of human leukocyte elastase (HLE) enzyme	B	4.4	pIC50	<40000	nM	IC50	J Med Chem (1990) 33: 2513-2521 [PMID:2391691]

ChEMBL data shown on this page come from version 32:

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]