Found 21 hits Enz. Inhib. hit(s) with Target = 'Glutamate carboxypeptidase 2' and Ligand = 'BDBM17659' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.200 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description Concentration of the compound required for the neuroprotective effect determined by inhibition of GCP II |
Bioorg Med Chem Lett 13: 2097-100 (2003)
BindingDB Entry DOI: 10.7270/Q2Z60NF2 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.200 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description In vitro inhibitory activity against glutamate carboxypeptidase II (GCP II) using N-acetyl-L-aspartyl-[3H]-L-glutamate as a substrate |
J Med Chem 46: 1989-96 (2003)
Article DOI: 10.1021/jm020515w BindingDB Entry DOI: 10.7270/Q2SQ8ZRG |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Rattus norvegicus) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.275 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
ZENECA Pharmaceuticals
Curated by ChEMBL
| Assay Description Compound was tested for inhibition of the Folate hydrolase |
J Med Chem 39: 619-22 (1996)
Article DOI: 10.1021/jm950801q BindingDB Entry DOI: 10.7270/Q2FN16V8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.280 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Academy of Sciences of the Czech Republic
Curated by ChEMBL
| Assay Description Inhibition of antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic ... |
J Med Chem 58: 4357-63 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00278 BindingDB Entry DOI: 10.7270/Q2DR2X70 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.300 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Bayer HealthCare
Curated by ChEMBL
| Assay Description Binding affinity to NAALADase |
J Med Chem 55: 9510-20 (2012)
Article DOI: 10.1021/jm300710j BindingDB Entry DOI: 10.7270/Q28053R3 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 0.400 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Bayer HealthCare
Curated by ChEMBL
| Assay Description Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid ... |
J Med Chem 55: 9510-20 (2012)
Article DOI: 10.1021/jm300710j BindingDB Entry DOI: 10.7270/Q28053R3 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 6.60 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Siemens Medical Solutions USA, Inc.
US Patent
| Assay Description The inhibitory activity of all compounds was determined using a fluorescent assay of human PSMA activity. The enzyme used in the assay was purchased ... |
US Patent US10894807 (2021)
BindingDB Entry DOI: 10.7270/Q2SN0D25 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| 31 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto University
Curated by ChEMBL
| Assay Description Displacement of [123I]-DCIT from PSMA in human LNCaP cells after 1 hr by gamma counting |
J Med Chem 56: 7890-901 (2013)
Article DOI: 10.1021/jm400895s BindingDB Entry DOI: 10.7270/Q21G0NPK |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Johns Hopkins School of Medicine
Curated by ChEMBL
| Assay Description Inhibition of GCP-2 (unknown origin) |
Drug Metab Dispos 40: 2315-23 (2012)
Article DOI: 10.1124/dmd.112.046821 BindingDB Entry DOI: 10.7270/Q2W66NG5 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description Inhibition of N-acetyl-L-aspartyl-[3H]-L-glutamate binding to glutamate carboxypeptidase II (GCP II) |
J Med Chem 46: 1989-96 (2003)
Article DOI: 10.1021/jm020515w BindingDB Entry DOI: 10.7270/Q2SQ8ZRG |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Rattus norvegicus) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description Inhibitory concentration against rat brain NAALADase (Folate hydrolase) |
J Med Chem 44: 4170-5 (2001)
BindingDB Entry DOI: 10.7270/Q2D21WX8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description Inhibition of Glutamate carboxypeptidase II |
Bioorg Med Chem Lett 13: 2097-100 (2003)
BindingDB Entry DOI: 10.7270/Q2Z60NF2 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Notre Dame
Curated by ChEMBL
| Assay Description Inhibition of human recombinant NAALADase |
Bioorg Med Chem 16: 1648-57 (2008)
Article DOI: 10.1016/j.bmc.2007.11.030 BindingDB Entry DOI: 10.7270/Q2MC90VM |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
Bayer HealthCare
Curated by ChEMBL
| Assay Description Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid ... |
J Med Chem 55: 9510-20 (2012)
Article DOI: 10.1021/jm300710j BindingDB Entry DOI: 10.7270/Q28053R3 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Rattus norvegicus) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 5.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Inhibitory activity of the compound against expressed rat Glutamate carboxypeptidase II, using a substrate concentration of 5 microM |
J Med Chem 44: 298-301 (2001)
BindingDB Entry DOI: 10.7270/Q2KD1X7Q |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 52 | n/a | n/a | n/a | n/a | n/a | n/a |
McMaster University
Curated by ChEMBL
| Assay Description Displacement of [125I]23 from PSMA in human LNCAP cells |
J Med Chem 59: 2660-73 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01881 BindingDB Entry DOI: 10.7270/Q2X068XP |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 80 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.0c01935 BindingDB Entry DOI: 10.7270/Q2NS0ZWP |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | 80 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113936 BindingDB Entry DOI: 10.7270/Q2V69PKR |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | n/a | 0.5 | n/a | n/a | n/a | n/a | n/a |
Justus-Liebig-Universitat Giessen
Curated by ChEMBL
| Assay Description Binding affinity to PSMA in human PC3 cells assessed as cell surface binding in Tris-buffered saline buffer |
J Med Chem 52: 544-50 (2009)
Article DOI: 10.1021/jm801033c BindingDB Entry DOI: 10.7270/Q2MW2H04 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | n/a | 0.400 | n/a | n/a | n/a | n/a | n/a |
Justus-Liebig-Universitat Giessen
Curated by ChEMBL
| Assay Description Binding affinity to PSMA in human LNCaP cells assessed as cell surface binding in Tris-buffered saline buffer |
J Med Chem 52: 544-50 (2009)
Article DOI: 10.1021/jm801033c BindingDB Entry DOI: 10.7270/Q2MW2H04 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Glutamate carboxypeptidase 2
(Homo sapiens (Human)) | BDBM17659
((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)Show InChI InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13) | PDB MMDB
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| n/a | n/a | n/a | n/a | 0.620 | n/a | n/a | n/a | n/a |
Guilford Pharmaceuticals Inc.
Curated by ChEMBL
| Assay Description Concentration of the compound required for the neuroprotective effect determined by inhibition of GCP II |
Bioorg Med Chem Lett 13: 2097-100 (2003)
BindingDB Entry DOI: 10.7270/Q2Z60NF2 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |