Target Validation Information
TTD ID	T97071
Target Name	Glutamate carboxypeptidase II (GCPII)
Type of Target	Successful
Drug Potency against Target	2-(2-carboxy-5-mercaptopentyl)benzoic acid	Drug Info	IC50 = 1700 nM	[3]
	2-(2-carboxy-7-mercaptoheptyl)benzoic acid	Drug Info	IC50 = 190 nM	[3]
	2-(2-Hydroxycarbamoyl-ethyl)-pentanedioic acid	Drug Info	IC50 = 1200 nM	[2]
	2-(2-Mercapto-ethyl)-pentanedioic acid	Drug Info	IC50 = 580 nM	[1]
	2-(2-Phosphonooxy-ethyl)-pentanedioic acid	Drug Info	IC50 = 1200 nM	[1]
	2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid	Drug Info	IC50 = 2200 nM	[3]
	2-(3-carboxybenzyl)succinic acid	Drug Info	IC50 = 15000 nM	[3]
	2-(3-cyanobenzyl)-5-mercaptopentanoic acid	Drug Info	IC50 = 1800 nM	[3]
	2-(3-Hydroxycarbamoyl-propyl)-pentanedioic acid	Drug Info	IC50 = 940 nM	[2]
	2-(3-Mercapto-propyl)-pentanedioic acid	Drug Info	IC50 = 90 nM	[1]
	2-(3-Methylsulfanyl-propyl)-pentanedioic acid	Drug Info	IC50 = 6500 nM	[1]
	2-(4-Mercapto-butyl)-pentanedioic acid	Drug Info	IC50 = 1100 nM	[1]
	2-(5-Mercapto-pentyl)-pentanedioic acid	Drug Info	IC50 = 2600 nM	[1]
	2-benzyl-5-mercaptopentanoic acid	Drug Info	IC50 = 1400 nM	[3]
	2-Hydroxycarbamoyl-pentanedioic acid	Drug Info	IC50 = 4000 nM	[2]
	2-Hydroxycarbamoylmethyl-pentanedioic acid	Drug Info	IC50 = 220 nM	[2]
	2-Mercapto-pentanedioic acid	Drug Info	IC50 = 2600 nM	[1]
	2-Mercaptomethyl-pentanedioic acid	Drug Info	IC50 = 6000 nM	[1]
	2-Phosphonooxy-pentanedioic acid	Drug Info	IC50 = 1400 nM	[1]
	2-PMPA	Drug Info	IC50 = 0.3 nM	[5]
	3-(1-carboxy-4-mercaptobutoxy)benzoic acid	Drug Info	IC50 = 14 nM	[3]
	3-(2-carbamoyl-5-mercaptopentyl)benzoic acid	Drug Info	IC50 = 640 nM	[3]
	3-(2-carboxy-3-mercaptopropyl)benzoic acid	Drug Info	IC50 = 440 nM	[3]
	3-(2-carboxy-3-phosphonopropyl)benzoic acid	Drug Info	IC50 = 120 nM	[3]
	3-(2-carboxy-4-mercaptobutyl)benzoic acid	Drug Info	IC50 = 1100 nM	[3]
	3-(2-carboxy-5-mercaptopentyl)benzoic acid	Drug Info	IC50 = 15 nM	[3]
	3-(2-carboxy-6-mercaptohexyl)benzoic acid	Drug Info	IC50 = 390 nM	[3]
	3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid	Drug Info	IC50 = 32 nM	[3]
	4-(2-carboxy-5-mercaptopentyl)benzoic acid	Drug Info	IC50 = 63 nM	[3]
	5-Mercapto-pentanoic acid	Drug Info	IC50 = 1400 nM	[1]
	[3H]quisqualate	Drug Info	IC50 = 9500 nM	[4]
References
REF 1	Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J Med Chem. 2003 May 8;46(10):1989-96.
REF 2	Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.
REF 3	Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain. J Med Chem. 2006 May 18;49(10):2876-85.
REF 4	Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. J Med Chem. 2007 Jul 12;50(14):3267-73.
REF 5	Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer. Bioorg Med Chem. 2008 Feb 15;16(4):1648-57.

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