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Literature summary for 3.4.17.21 extracted from

  • Majer, P.; Hin, B.; Stoermer, D.; Adams, J.; Xu, W.; Duvall, B.R.; Delahanty, G.; Liu, Q.; Stathis, M.J.; Wozniak, K.M.; Slusher, B.S.; Tsukamoto, T.
    Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1 side chain (2006), J. Med. Chem., 49, 2876-2885.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(2-carboxy-5-mercaptopentyl)benzoic acid IC50: 1700 nM Homo sapiens
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid IC50: 2200 nM Homo sapiens
2-(3-carboxybenyl)succinic acid IC50: 0.015 mM Homo sapiens
2-(3-cyanobenzyl)-5-mercaptopentanoic acid IC50: 1800 nM Homo sapiens
2-(3-mercaptopropyl)-pentanedioic acid i.e. 2-MPPA, IC50: 90 nM Homo sapiens
2-benzyl-5-mercaptopentanoic acid IC50: 1400 nM Homo sapiens
3-(1-carboxy-4-mercaptobutoxy)benzoic acid IC50: 14 nM Homo sapiens
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid IC50: 640 nM Homo sapiens
3-(2-carboxy-3-hydroxycarbamoylpropyl)benzoic acid IC50: 0.015 mM Homo sapiens
3-(2-carboxy-3-phosphonopropyl)benzoic acid IC50: 120 nM Homo sapiens
3-(2-carboxy-5-mercaptopentyl)benzoic acid IC50: 15 nM Homo sapiens
3-(2-carboxy-5-mercaptopentyl)benzoic acid methyl ester IC50: 2700 nM Homo sapiens
3-(2-carboxy-5-mercaptosulfanylpentyl)benzoic acid IC50: 0.02 mM Homo sapiens
3-(2-carboxy-5-tritylsulfanylpentyl)benzoic acid IC50: 0.02 mM Homo sapiens
3-(5-mercapto-2-methoxycarbonylpentyl)benzoic acid IC50: 730 nM Homo sapiens
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid IC50: 32 nM Homo sapiens
3-[2-carboxy-3-(hydroxypentafluorophenylmethylphosphinoyl)propyl]benzoic acid IC50: 2400 nM Homo sapiens
4-(2-carboxy-5-mercaptopentyl)benzoic acid IC50: 63 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O i.e. NAAG Homo sapiens N-acetyl-alpha-L-aspartate + L-glutamate
-
?

Synonyms

Synonyms Comment Organism
GCP II
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
IC50: 14 nM Homo sapiens 3-(1-carboxy-4-mercaptobutoxy)benzoic acid
0.000015
-
IC50: 15 nM Homo sapiens 3-(2-carboxy-5-mercaptopentyl)benzoic acid
0.000032
-
IC50: 32 nM Homo sapiens 3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid
0.000063
-
IC50: 63 nM Homo sapiens 4-(2-carboxy-5-mercaptopentyl)benzoic acid
0.00009
-
i.e. 2-MPPA, IC50: 90 nM Homo sapiens 2-(3-mercaptopropyl)-pentanedioic acid
0.00012
-
IC50: 120 nM Homo sapiens 3-(2-carboxy-3-phosphonopropyl)benzoic acid
0.00064
-
IC50: 640 nM Homo sapiens 3-(2-carbamoyl-5-mercaptopentyl)benzoic acid
0.00073
-
IC50: 730 nM Homo sapiens 3-(5-mercapto-2-methoxycarbonylpentyl)benzoic acid
0.0014
-
IC50: 1400 nM Homo sapiens 2-benzyl-5-mercaptopentanoic acid
0.0017
-
IC50: 1700 nM Homo sapiens 2-(2-carboxy-5-mercaptopentyl)benzoic acid
0.0018
-
IC50: 1800 nM Homo sapiens 2-(3-cyanobenzyl)-5-mercaptopentanoic acid
0.0022
-
IC50: 2200 nM Homo sapiens 2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid
0.0024
-
IC50: 2400 nM Homo sapiens 3-[2-carboxy-3-(hydroxypentafluorophenylmethylphosphinoyl)propyl]benzoic acid
0.0027
-
IC50: 2700 nM Homo sapiens 3-(2-carboxy-5-mercaptopentyl)benzoic acid methyl ester
0.015
-
IC50: 0.015 mM Homo sapiens 3-(2-carboxy-3-hydroxycarbamoylpropyl)benzoic acid
0.015
-
IC50: 0.015 mM Homo sapiens 2-(3-carboxybenyl)succinic acid
0.02
-
IC50: 0.02 mM Homo sapiens 3-(2-carboxy-5-mercaptosulfanylpentyl)benzoic acid
0.02
-
IC50: 0.02 mM Homo sapiens 3-(2-carboxy-5-tritylsulfanylpentyl)benzoic acid