Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T38179 | Target Info | |||
| Target Name | Staphylococcus Beta-lactamase (Stap-coc blaZ) | ||||
| Synonyms |
blaZ; Cephalosporinase
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| Target Type | Successful Target | ||||
| Gene Name | Stap-coc blaZ | ||||
| Biochemical Class | Carbon-nitrogen hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Tazobactam sodium
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Investigative | Compound Info | ||
| Synonyms |
Tazobactam sodium salt; UNII-UXA545ABTT; Tazobactam (sodium); CL-307579; UXA545ABTT; CHEMBL1439; CL 307579; CL 307,579; 89785-84-2 (sodium); YTR 830; Tazobactam sodium [USAN]; DSSTox_CID_26030; DSSTox_RID_81299; DSSTox_GSID_46030; CL-298741; YTR-830; tazobactum; NCGC00159340-02; SCHEMBL259991; Tazobactam sodium (JAN/USAN); DTXSID8046030; YP-14; Tox21_111584; BDBM50157692; AKOS015962921; AKOS016843926; Tox21_111584_1; CS-W009884; HY-W009168; NCGC00159340-05; AC-18978; AC-32478; AS-56873; Tazobactam sodium salt, analytical standard; D03707; T-1446; Tazobactam sodium salt, beta-lactamase inhibitor; Q27158392; Tazobactam sodium salt, Antibiotic for Culture Media Use Only
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| Activity |
IC50 = 51900 nM
|
[1] | |||
| Compound Name |
2-Methylene-3-methyl-4-(sodiooxycarbonyl)-7-[(Z)-2-oxo-2-tert-butoxyethylidene]cepham-3-ene 1,1-dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL355648
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| Activity |
IC50 = 56500 nM
|
[2] | |||
| Compound Name |
Sodium;(7Z)-3-[[2-(3,4-dihydroxyphenyl)acetyl]oxymethyl]-5,5,8-trioxo-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL169303
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| Activity |
IC50 = 67000 nM
|
[3] | |||
| Compound Name |
2,3-Dimethyl-4-(sodiooxycarbonyl)-7-[(Z)-(2-pyridinyl)methylene]cepham-3-ene 1,1-dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL435467
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| Activity |
IC50 = 74100 nM
|
[2] | |||
| Compound Name |
Sodium;(7Z)-3-[(1E)-buta-1,3-dienyl]-5,5,8-trioxo-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL167311
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| Activity |
IC50 = 75000 nM
|
[3] | |||
| Compound Name |
Disodium;(2S,3R,6Z)-3-(acetyloxymethyl)-6-(carboxylatomethylidene)-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL61762
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| Activity |
IC50 = 76530 nM
|
[1] | |||
| Compound Name |
2-Methylene-3-methyl-4-(sodiooxycarbonyl)-7-[(Z)-(2-pyridinyl)methylene]cepham-3-ene 1,1-dioxide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL166730
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| Activity |
IC50 = 91100 nM
|
[2] | |||
| Compound Name |
2-Methylene-3-(acetoxymethyl)-4-(sodiooxycarbonyl)-7-[(Z)-(2-pyridinyl)methylene]cepham-3-ene 1,1-dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL353004
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| Activity |
IC50 = 99200 nM
|
[2] | |||
| Compound Name |
Sodium;(7Z)-5,5,8-trioxo-3-[(2-phenoxyacetyl)oxymethyl]-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL422212
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| Activity |
IC50 = 100000 nM
|
[3] | |||
| Compound Name |
Disodium;(2S,6Z)-6-(carboxylatomethylidene)-3,3-dimethyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL60491
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|
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| Activity |
IC50 = 108000 nM
|
[1] | |||
| Compound Name |
Sodium;(7Z)-5,5,8-trioxo-3-(prop-2-enoyloxymethyl)-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL169154
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|
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| Activity |
IC50 = 110000 nM
|
[3] | |||
| Compound Name |
Disodium;(2S,3R,6Z)-6-(carboxylatomethylidene)-3-[[2-(3,4-dihydroxyphenyl)acetyl]oxymethyl]-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL305361
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|
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| Activity |
IC50 = 116000 nM
|
[1] | |||
| Compound Name |
Disodium;(2S,3R,6Z)-6-(carboxylatomethylidene)-3-(chloromethyl)-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL59227
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|
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| Activity |
IC50 = 120500 nM
|
[1] | |||
| Compound Name |
Sodium;(7Z)-3-[(E)-3-amino-3-oxoprop-1-enyl]-5,5,8-trioxo-7-(thiophen-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL353694
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|
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| Activity |
IC50 = 154000 nM
|
[3] | |||
| Compound Name |
2-[Bis(methylthio)methylene]-3-methyl-4-(sodiooxycarbonyl)-7-[(Z)-(2-pyridinyl)methylene]cepham-3-ene 1,1-dioxide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL171001
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|
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| Activity |
IC50 = 173000 nM
|
[2] | |||
| Compound Name |
Disodium;(2S,3R,6Z)-6-(carboxylatomethylidene)-3-(formyloxymethyl)-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL61760
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|
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| Activity |
IC50 = 173000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 11 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Methylene-3-(acetoxymethyl)-4-(sodiooxycarbonyl)-7-[(Z)-2-oxo-2-(sodiooxy)ethylidene]cepham-3-ene 1,1-dioxide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL355571
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|
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| Activity |
IC50 = 230000 nM
|
[2] | |||
| Compound Name |
Sodium;(7Z)-3-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]-5,5,8-trioxo-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL353230
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|
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| Activity |
IC50 = 240000 nM
|
[3] | |||
| Compound Name |
2-Methylene-3-methyl-4-(sodiooxycarbonyl)-7-[(Z)-2-oxo-2-(sodiooxy)ethylidene]cepham-3-ene 1,1-dioxide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL166677
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|
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| Activity |
IC50 = 277000 nM
|
[2] | |||
| Compound Name |
Sodium;(7Z)-3-cyano-5,5,8-trioxo-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL355288
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|
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| Activity |
IC50 = 280000 nM
|
[3] | |||
| Compound Name |
[3-(Acetyloxymethyl)-7-[(Z)-2-pyridylmethylene]cepham-3-ene-4-carboxylic acid sodium]1,1-dioxide salt
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL268632
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|
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| Activity |
IC50 = 402000 nM
|
[2] | |||
| Compound Name |
Sodium;(2S,3R,6Z)-3-(chloromethyl)-6-(2-methoxy-2-oxoethylidene)-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL292147
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|
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| Activity |
IC50 = 432000 nM
|
[1] | |||
| Compound Name |
Disodium;(2S,3S,6Z)-6-(carboxylatomethylidene)-3-[(E)-2-cyanoethenyl]-3-methyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL60220
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|
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| Activity |
IC50 = 504000 nM
|
[1] | |||
| Compound Name |
Disodium;(2S,3R,6Z)-6-(carboxylatomethylidene)-3-methyl-4,4,7-trioxo-3-[(2-phenylacetyl)oxymethyl]-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL292093
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|
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| Activity |
IC50 = 579000 nM
|
[1] | |||
| Compound Name |
Sodium;(4S,6R,7Z)-3-methyl-4-(1-methyltetrazol-5-yl)sulfanyl-5,5,8-trioxo-7-(pyridin-2-ylmethylidene)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL355246
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|
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| Activity |
IC50 = 844000 nM
|
[2] | |||
| Compound Name |
Sodium;(2S,3R,6Z)-6-(2-methoxy-2-oxoethylidene)-3-methyl-3-[[2-(1-methyltetrazol-5-yl)sulfanylacetyl]oxymethyl]-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL59053
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|
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| Activity |
IC50 = 939700 nM
|
[1] | |||
| Compound Name |
[3-(Acetyloxymethyl)-7-[(Z)-tert-butoxycarbonylmethylene]cepham-3-ene-4-carboxylic acid sodium]1,1-dioxide salt
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL268919
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|
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| Activity |
IC50 = 977000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1997-2002. | ||||
| REF 2 | The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors. Bioorg Med Chem Lett. 2000 May 1;10(9):847-51. | ||||
| REF 3 | The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors. Bioorg Med Chem Lett. 2000 May 1;10(9):853-7. | ||||
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