Target
Glutamate carboxypeptidase 2 [44-750]
Ligand
BDBM17659
Substrate
BDBM17658
Meas. Tech.
Microplate GCPII Radioactivity-Based Assay
pH
7.4±n/a
Temperature
310.15±n/a K
IC50
0.3±0.05 nM
Citation
 Majer, PHin, BStoermer, DAdams, JXu, WDuvall, BRDelahanty, GLiu, QStathis, MJWozniak, KMSlusher, BSTsukamoto, T Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain. J Med Chem 49:2876-85 (2006) [PubMed]  Article 
Target
Name:
Glutamate carboxypeptidase 2 [44-750]
Synonyms:
FOLH | FOLH1 | FOLH1_HUMAN | Folate hydrolase 1 | Folylpoly-gamma-glutamate carboxypeptidase | Glutamate Carboxypeptidase II (GCPII) | Glutamate carboxypeptidase 2 | Membrane glutamate carboxypeptidase | NAALAD1 | PSM | PSMA | Prostate-specific membrane antigen | Prostate-specific membrane antigen (PSMA) | Pteroylpoly-gamma-glutamate carboxypeptidase | mGCP
Type:
Enzyme
Mol. Mass.:
79524.51
Organism:
Homo sapiens (Human)
Description:
The extracellular domain of human glutamate carboxypeptidase II (rhGCPII, amino acids 44-750) was overexpressed in Drosophila Schneider S2 cells and purified to homogeneity.
Residue:
707
Sequence:
KSSNEATNITPKHNMKAFLDELKAENIKKFLYNFTQIPHLAGTEQNFQLAKQIQSQWKEFGLDSVELAHYDVLLSYPNKTHPNYISIINEDGNEIFNTSLFEPPPPGYENVSDIVPPFSAFSPQGMPEGDLVYVNYARTEDFFKLERDMKINCSGKIVIARYGKVFRGNKVKNAQLAGAKGVILYSDPADYFAPGVKSYPDGWNLPGGGVQRGNILNLNGAGDPLTPGYPANEYAYRRGIAEAVGLPSIPVHPIGYYDAQKLLEKMGGSAPPDSSWRGSLKVPYNVGPGFTGNFSTQKVKMHIHSTNEVTRIYNVIGTLRGAVEPDRYVILGGHRDSWVFGGIDPQSGAAVVHEIVRSFGTLKKEGWRPRRTILFASWDAEEFGLLGSTEWAEENSRLLQERGVAYINADSSIEGNYTLRVDCTPLMYSLVHNLTKELKSPDEGFEGKSLYESWTKKSPSPEFSGMPRISKLGSGNDFEVFFQRLGIASGRARYTKNWETNKFSGYPLYHSVYETYELVEKFYDPMFKYHLTVAQVRGGMVFELANSIVLPFDCRDYAVVLRKYADKIYSISMKHPQEMKTYSVSFDSLFSAVKNFTEIASKFSERLQDFDKSNPIVLRMMNDQLMFLERAFIDPLGLPDRPFYRHVIYAPSSHNKYAGESFPGIYDALFDIESKVDPSKAWGEVKRQIYVAAFTVQAAAETLSEVA
  
Inhibitor
Name:
BDBM17659
Synonyms:
(R,S)-2-phosphonomethylpentanedioic acid | 2-(phosphonomethyl)pentanedioic acid | 2-PMPA | CHEMBL47009 | US10894807, ID P009 | pentanedioic acid analogue, (RS)-1
Type:
Small organic molecule
Emp. Form.:
C6H11O7P
Mol. Mass.:
226.1211
SMILES:
OC(=O)CCC(CP(O)(O)=O)C(O)=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM17658
Synonyms:
(2S)-2-[(3S)-3-acetamido-3-formamidopropanoic acid]pentanedioic acid | N-acetylaspartylglutamate (NAAG) | NAAG | [3H]NAAG
Type:
Small organic molecule
Emp. Form.:
C11H16N2O8
Mol. Mass.:
304.2533
SMILES:
CC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(O)=O |r|
Structure:
Search PDB for entries with ligand similarity: