Reaction Details Report a problem with these data
Target
Glutamate carboxypeptidase 2 [44-750]
Ligand
BDBM17754
Substrate
BDBM17658
Meas. Tech.
Microplate GCPII Radioactivity-Based Assay
pH
7.4±n/a
Temperature
310.15±n/a K
IC50
34±18 nM
Km
130±40 nM
kcat
4±2 1/sec
Citation
 Tsukamoto, T; Majer, P; Vitharana, D; Ni, C; Hin, B; Lu, XC; Thomas, AG; Wozniak, KM; Calvin, DC; Wu, Y; Slusher, BS; Scarpetti, D; Bonneville, GW Enantiospecificity of glutamate carboxypeptidase II inhibition. J Med Chem 48:2319-24 (2005) [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:
BDBM17754
Synonyms:
(2S)-2-({hydroxy[(2,3,4,5,6-pentafluorophenyl)methyl]phosphoryl}methyl)pentanedioic acid | pentanedioic acid analogue, (S)-2
Type:
Small organic molecule
Emp. Form.:
C13H12F5O6P
Mol. Mass.:
390.1966
SMILES:
OC(=O)CC[C@H](CP(O)(=O)Cc1c(F)c(F)c(F)c(F)c1F)C(O)=O |r|
Structure:
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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:
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