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Literature summary for 3.4.24.63 extracted from
- First insight into structure-activity relationships of selective meprin beta inhibitors (2017), Bioorg. Med. Chem. Lett., 27, 2428-2431 .
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | the astacin protease meprin beta is an emerging drug target for treatment of disorders such as kidney failure, fibrosis or inflammatory bowel disease | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (4-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]phenyl)acetic acid | - |
Homo sapiens |  |
| 3-([(1,3-benzodioxol-5-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 3-([(biphenyl-4-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 3-([[(3-fluoro-4-methoxyphenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 3-([[(4-carboxyphenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 3-([[(4-fluorophenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 3-([[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]methyl)benzoic acid | not only a potent inhibitor of meprin beta, but also a very potent inhibitor of MMP2, 9 and 13 | Homo sapiens | |
| 3-[(3-carboxybenzyl)[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | - |
Homo sapiens | |
| 3-[([2-(hydroxyamino)-2-oxoethyl][[4-(trifluoromethoxy)phenyl]sulfonyl]amino)methyl]benzoic acid | - |
Homo sapiens | |
| 3-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | - |
Homo sapiens | |
| 3-[[3-(hydroxyamino)-3-oxopropyl]sulfamoyl]benzoic acid | - |
Homo sapiens | |
| 4-([[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]methyl)benzoic acid | - |
Homo sapiens | |
| 4-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | - |
Homo sapiens | |
| actinonin | - |
Homo sapiens | |
| additional information | structure-activity relationships of selective meprin beta inhibitors, synthesis and inhibitory potency, overview. Preference of meprin beta for acidic residues in the P1' position. Acidic modifications induce potent inhibition and over 100fold selectivity over other structurally related metalloproteases such as MMP-2 or ADAM10 | Homo sapiens | |
| N-hydroxy-N2-(4-methoxybenzyl)-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(2-methoxy-4-methylphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(3-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4'-methoxybiphenyl-4-yl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(2-phenylethyl)glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(3-methylbutyl)glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-methylglycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-hydroxy-N2-[(4-phenoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N-isobutyl-N-(4-methoxyphenylsulfonyl)glycyl hydroxamic acid | NNGH | Homo sapiens | |
| N-[2-(hydroxyamino)-2-oxoethyl]-N-[(4-methoxyphenyl)sulfonyl]-beta-alanine | - |
Homo sapiens | |
| N2-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N2-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-(bicyclo[2.2.1]hept-2-ylmethyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N2-(biphenyl-4-ylsulfonyl)-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-benzyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N2-butyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N2-ethyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | - |
Homo sapiens | |
| N2-[(2,4-dimethylphenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(3,4-dimethoxyphenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(3,5-dichloro-4-hydroxyphenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(3-fluoro-4-methoxyphenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(4'-fluorobiphenyl-4-yl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(4-chlorophenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(4-fluorophenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[(5-chloro-2-methylphenyl)sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl]-N-hydroxyglycinamide | - |
Homo sapiens | |
| N3-[(3-chloro-4-hydroxyphenyl)sulfonyl]-N-hydroxy-b-alaninamide | - |
Homo sapiens | |
| NF449 | a potent and partially selective inhibitor | Homo sapiens | |
| PPNDS | a potent and partially selective inhibitor | Homo sapiens | |
| [[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]acetic acid | - |
Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | a zinc metalloproteinase | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q16820 | - |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| meprin beta | - |
Homo sapiens |
| metalloprotease meprin beta | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000008 | - |
PPNDS | pH and temperature not specified in the publication | Homo sapiens | |
| 0.000022 | - |
NF449 | pH and temperature not specified in the publication | Homo sapiens | |
| 0.002 | - |
actinonin | pH and temperature not specified in the publication | Homo sapiens | |
| 0.0074 | - |
N-isobutyl-N-(4-methoxyphenylsulfonyl)glycyl hydroxamic acid | pH and temperature not specified in the publication | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00006 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]methyl)benzoic acid | |
| 0.00006 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(3-carboxybenzyl)[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | |
| 0.00022 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[[3-(hydroxyamino)-3-oxopropyl]sulfamoyl]benzoic acid | |
| 0.00027 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([(1,3-benzodioxol-5-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | |
| 0.00031 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | |
| 0.00032 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([[(4-carboxyphenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | |
| 0.00034 | - |
pH and temperature not specified in the publication | Homo sapiens | (4-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]phenyl)acetic acid | |
| 0.0004 | - |
pH and temperature not specified in the publication | Homo sapiens | N3-[(3-chloro-4-hydroxyphenyl)sulfonyl]-N-hydroxy-b-alaninamide | |
| 0.00041 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]benzoic acid | |
| 0.00043 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(3,5-dichloro-4-hydroxyphenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.00065 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([[(3-fluoro-4-methoxyphenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | |
| 0.0007 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[([2-(hydroxyamino)-2-oxoethyl][[4-(trifluoromethoxy)phenyl]sulfonyl]amino)methyl]benzoic acid | |
| 0.00098 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-([[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]methyl)benzoic acid | |
| 0.00106 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([[(4-fluorophenyl)sulfonyl][2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | |
| 0.00108 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-([(biphenyl-4-ylsulfonyl)[2-(hydroxyamino)-2-oxoethyl]amino]methyl)benzoic acid | |
| 0.00193 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.00255 | - |
pH and temperature not specified in the publication | Homo sapiens | N-[2-(hydroxyamino)-2-oxoethyl]-N-[(4-methoxyphenyl)sulfonyl]-beta-alanine | |
| 0.00385 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-(biphenyl-4-ylsulfonyl)-N-hydroxyglycinamide | |
| 0.00442 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4'-methoxybiphenyl-4-yl)sulfonyl]glycinamide | |
| 0.00503 | - |
pH and temperature not specified in the publication | Homo sapiens | (4-[[2-(hydroxyamino)-2-oxoethyl]sulfamoyl]phenyl)acetic acid | |
| 0.00565 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-hydroxyglycinamide | |
| 0.00598 | - |
pH and temperature not specified in the publication | Homo sapiens | [[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]acetic acid | |
| 0.00619 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(3-fluoro-4-methoxyphenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.00731 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(4'-fluorobiphenyl-4-yl)sulfonyl]-N-hydroxyglycinamide | |
| 0.00742 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-N-hydroxyglycinamide | |
| 0.00902 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.01026 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl]-N-hydroxyglycinamide | |
| 0.01432 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(4-fluorophenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.01477 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(2,4-dimethylphenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.01717 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(4-chlorophenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.01797 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(5-chloro-2-methylphenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.0188 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4-phenoxyphenyl)sulfonyl]glycinamide | |
| 0.01885 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(3-methoxyphenyl)sulfonyl]glycinamide | |
| 0.0257 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(2-methoxy-4-methylphenyl)sulfonyl]glycinamide | |
| 0.0269 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-[(3,4-dimethoxyphenyl)sulfonyl]-N-hydroxyglycinamide | |
| 0.0312 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-ethyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.03253 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-methylglycinamide | |
| 0.03495 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-(4-methoxybenzyl)-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.0375 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-butyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.0388 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(3-methylbutyl)glycinamide | |
| 0.04047 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-benzyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
| 0.0429 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(2-phenylethyl)glycinamide | |
| 0.04387 | - |
pH and temperature not specified in the publication | Homo sapiens | N2-(bicyclo[2.2.1]hept-2-ylmethyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide | |
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