Target Validation Information
Target ID T97071
Target Name Glutamate carboxypeptidase II
Target Type
Successful
Drug Potency against Target 2-(3-Hydroxycarbamoyl-propyl)-pentanedioic acid Drug Info IC50 = 940 nM [526637]
2-(2-carboxy-5-mercaptopentyl)benzoic acid Drug Info IC50 = 1700 nM [528194]
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid Drug Info IC50 = 32 nM [528194]
3-(2-carboxy-4-mercaptobutyl)benzoic acid Drug Info IC50 = 1100 nM [528194]
4-(2-carboxy-5-mercaptopentyl)benzoic acid Drug Info IC50 = 63 nM [528194]
2-benzyl-5-mercaptopentanoic acid Drug Info IC50 = 1400 nM [528194]
3-(2-carboxy-6-mercaptohexyl)benzoic acid Drug Info IC50 = 390 nM [528194]
3-(2-carboxy-3-mercaptopropyl)benzoic acid Drug Info IC50 = 440 nM [528194]
2-(3-carboxybenzyl)succinic acid Drug Info IC50 = 15000 nM [528194]
3-(2-carboxy-3-phosphonopropyl)benzoic acid Drug Info IC50 = 120 nM [528194]
2-(3-cyanobenzyl)-5-mercaptopentanoic acid Drug Info IC50 = 1800 nM [528194]
3-(2-carboxy-5-mercaptopentyl)benzoic acid Drug Info IC50 = 15 nM [528194]
2-Phosphonooxy-pentanedioic acid Drug Info IC50 = 1400 nM [526615]
3-(1-carboxy-4-mercaptobutoxy)benzoic acid Drug Info IC50 = 14 nM [528194]
2-(2-Hydroxycarbamoyl-ethyl)-pentanedioic acid Drug Info IC50 = 1200 nM [526637]
2-(2-carboxy-7-mercaptoheptyl)benzoic acid Drug Info IC50 = 190 nM [528194]
QUISQUALATE Drug Info IC50 = 9500 nM [528891]
2-(5-Mercapto-pentyl)-pentanedioic acid Drug Info IC50 = 2600 nM [526615]
2-(3-Methylsulfanyl-propyl)-pentanedioic acid Drug Info IC50 = 6500 nM [526615]
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid Drug Info IC50 = 640 nM [528194]
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid Drug Info IC50 = 2200 nM [528194]
2-(2-Phosphonooxy-ethyl)-pentanedioic acid Drug Info IC50 = 1200 nM [526615]
2-Mercaptomethyl-pentanedioic acid Drug Info IC50 = 6000 nM [526615]
5-Mercapto-pentanoic acid Drug Info IC50 = 1400 nM [526615]
2-(3-Mercapto-propyl)-pentanedioic acid Drug Info IC50 = 90 nM [526615]
2-Hydroxycarbamoyl-pentanedioic acid Drug Info IC50 = 4000 nM [526637]
2-Hydroxycarbamoylmethyl-pentanedioic acid Drug Info IC50 = 220 nM [526637]
2-(phosphonomethyl)pentanedioic acid Drug Info IC50 = 0.3 nM [529200]
2-Mercapto-pentanedioic acid Drug Info IC50 = 2600 nM [526615]
2-(4-Mercapto-butyl)-pentanedioic acid Drug Info IC50 = 1100 nM [526615]
2-(2-Mercapto-ethyl)-pentanedioic acid Drug Info IC50 = 580 nM [526615]
References
Ref 526637Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 526637Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528891J Med Chem. 2007 Jul 12;50(14):3267-73. Epub 2007 Jun 14.Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 528194J Med Chem. 2006 May 18;49(10):2876-85.Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526637Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Ref 526637Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Ref 529200Bioorg Med Chem. 2008 Feb 15;16(4):1648-57. Epub 2007 Nov 17.Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Ref 526615J Med Chem. 2003 May 8;46(10):1989-96.Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.

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