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 526637 | Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. | ||||
Ref 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 528194 | J 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 526615 | J 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 528194 | J 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 526637 | Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. | ||||
Ref 528194 | J 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 528891 | J 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 526615 | J 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 526615 | J 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 528194 | J 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 528194 | J 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 526615 | J 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 526615 | J 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 526615 | J 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 526615 | J 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 526637 | Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. | ||||
Ref 526637 | Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. | ||||
Ref 529200 | Bioorg 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 526615 | J 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 526615 | J 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 526615 | J 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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