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Literature summary for 3.4.17.21 extracted from

  • Jackson, P.F.; Tays, K.L.; Maclin, K.M.; Ko, Y.S.; Li, W.; Vitharana, D.; Tsukamoto, T.; Stoermer, D.; Lu, X.C.; Wozniak, K.; Slusher, B.S.
    Design and pharmacological activity of phosphinic acid based NAALADase inhibitors (2001), J. Med. Chem., 44, 4170-4175.
    View publication on PubMed
Search for more literature for 3.4.17.21

Application

Application Comment Organism
medicine NAALADase inhibition may provide a new aproach for the treatment of both neurodegenerative disorders and peripheral neuropathies Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
2-(phosphonomethyl)-4-(5H-tetrazol-5-yl)butanoic acid IC50: 175 nM Rattus norvegicus
2-(phosphonomethyl)hexanedioic acid IC50: 185 nM Rattus norvegicus
2-(phosphonomethyl)pentanedioic acid IC50: 0.3 nM Rattus norvegicus
2-(phosphonomethyl)succinic acid IC50: 2200 nM Rattus norvegicus
2-([hydroxy[hydroxy(phenyl)methyl]phosphoryl]methyl)pentanedioic acid IC50: 55 nM Rattus norvegicus
2-([hydroxy[hydroxy(pyridin-4-yl)methyl]phosphoryl]methyl)pentanedioic acid IC50: 10 nM Rattus norvegicus
2-benzyl-3-phosphonopropanoic acid IC50: 548 nM Rattus norvegicus
2-[(hydroxy[[(4-methoxyphenyl)amino]methyl]phosphoryl)methyl]pentanedioic acid IC50: 3 nM Rattus norvegicus
2-[[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 0.5 nM Rattus norvegicus
2-[[(2-carboxy-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 2 nM Rattus norvegicus
2-[[(2-carboxypropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 1.5 nM Rattus norvegicus
2-[[(2-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 156 nM Rattus norvegicus
2-[[(3,5-difluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 49 nM Rattus norvegicus
2-[[(3-aminobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 143 nM Rattus norvegicus
2-[[(anilinomethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 4 nM Rattus norvegicus
2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 53 nM Rattus norvegicus
2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid IC50: 149 nM Rattus norvegicus
2-[[hydroxy(4-methoxybenzyl)phosphoryl]methyl]pentanedioic acid IC50: 90 nM Rattus norvegicus
2-[[hydroxy(4-methylbenzyl)phosphoryl]methyl]pentanedioic acid IC50: 68 nM Rattus norvegicus
2-[[hydroxy(pentafluorobenzyl)phosphoryl]methyl]pentanedioic acid IC50: 82 nM. Significantly prevents neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In the chronic constrictive model of neuropathic pain, the inhibitor sifnificantly attenuats the hypersensitivity observed with saline-treated animals Rattus norvegicus
2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid IC50: 2930 nM Rattus norvegicus
2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid IC50: 360 nM Rattus norvegicus
2-[[[(3-fluorophenyl)(hydroxy)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 16 nM Rattus norvegicus
2-[[[(benzylamino)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 59 nM Rattus norvegicus
2-[[[3,5-bis(trifluoromethyl)benzyl](hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 55 nM Rattus norvegicus
2-[[[3-(benzyloxy)-2-methyl-3-oxopropyl](hydroxy)phosphoryl]methyl]pentanedioic acid IC50: 95 nM Rattus norvegicus
4-(3-hydroxyphenyl)-2-(phosphonomethyl)butanoic acid IC50: 508 nM Rattus norvegicus
4-cyano-2-(phosphonomethyl)butanoic acid IC50: 335 nM Rattus norvegicus
4-phenyl-2-(phosphonomethyl)butanoic acid IC50: 199 nM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
NAALADase
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000003
-
 IC50: 0.3 nM Rattus norvegicus 2-(phosphonomethyl)pentanedioic acid
0.0000005
-
 IC50: 0.5 nM Rattus norvegicus 2-[[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.0000015
-
 IC50: 1.5 nM Rattus norvegicus 2-[[(2-carboxypropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000002
-
 IC50: 2 nM Rattus norvegicus 2-[[(2-carboxy-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000003
-
 IC50: 3 nM Rattus norvegicus 2-[(hydroxy[[(4-methoxyphenyl)amino]methyl]phosphoryl)methyl]pentanedioic acid
0.000004
-
 IC50: 4 nM Rattus norvegicus 2-[[(anilinomethyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.00001
-
 IC50: 10 nM Rattus norvegicus 2-([hydroxy[hydroxy(pyridin-4-yl)methyl]phosphoryl]methyl)pentanedioic acid
0.000016
-
 IC50: 16 nM Rattus norvegicus 2-[[[(3-fluorophenyl)(hydroxy)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
0.000049
-
 IC50: 49 nM Rattus norvegicus 2-[[(3,5-difluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000053
-
 IC50: 53 nM Rattus norvegicus 2-[[benzyl(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000055
-
 IC50: 55 nM Rattus norvegicus 2-[[[3,5-bis(trifluoromethyl)benzyl](hydroxy)phosphoryl]methyl]pentanedioic acid
0.000055
-
 IC50: 55 nM Rattus norvegicus 2-([hydroxy[hydroxy(phenyl)methyl]phosphoryl]methyl)pentanedioic acid
0.000059
-
 IC50: 59 nM Rattus norvegicus 2-[[[(benzylamino)methyl](hydroxy)phosphoryl]methyl]pentanedioic acid
0.000068
-
 IC50: 68 nM Rattus norvegicus 2-[[hydroxy(4-methylbenzyl)phosphoryl]methyl]pentanedioic acid
0.000082
-
 IC50: 82 nM. Significantly prevents neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In the chronic constrictive model of neuropathic pain, the inhibitor sifnificantly attenuats the hypersensitivity observed with saline- Rattus norvegicus 2-[[hydroxy(pentafluorobenzyl)phosphoryl]methyl]pentanedioic acid
0.00009
-
 IC50: 90 nM Rattus norvegicus 2-[[hydroxy(4-methoxybenzyl)phosphoryl]methyl]pentanedioic acid
0.000095
-
 IC50: 95 nM Rattus norvegicus 2-[[[3-(benzyloxy)-2-methyl-3-oxopropyl](hydroxy)phosphoryl]methyl]pentanedioic acid
0.000143
-
 IC50: 143 nM Rattus norvegicus 2-[[(3-aminobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000149
-
 IC50: 149 nM Rattus norvegicus 2-[[hydroxy(2-phenylethyl)phosphoryl]methyl]pentanedioic acid
0.000156
-
 IC50: 156 nM Rattus norvegicus 2-[[(2-fluorobenzyl)(hydroxy)phosphoryl]methyl]pentanedioic acid
0.000175
-
 IC50: 175 nM Rattus norvegicus 2-(phosphonomethyl)-4-(5H-tetrazol-5-yl)butanoic acid
0.000185
-
 IC50: 185 nM Rattus norvegicus 2-(phosphonomethyl)hexanedioic acid
0.000199
-
 IC50: 199 nM Rattus norvegicus 4-phenyl-2-(phosphonomethyl)butanoic acid
0.000335
-
 IC50: 335 nM Rattus norvegicus 4-cyano-2-(phosphonomethyl)butanoic acid
0.00036
-
 IC50: 360 nM Rattus norvegicus 2-[[hydroxy(propyl)phosphoryl]methyl]pentanedioic acid
0.000508
-
 IC50: 508 nM Rattus norvegicus 4-(3-hydroxyphenyl)-2-(phosphonomethyl)butanoic acid
0.000548
-
 IC50: 548 nM Rattus norvegicus 2-benzyl-3-phosphonopropanoic acid
0.0022
-
 IC50: 2200 nM Rattus norvegicus 2-(phosphonomethyl)succinic acid
0.00293
-
 IC50: 2930 nM Rattus norvegicus 2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid