Reaction Details Report a problem with these data
Target
Glutamate carboxypeptidase 2 [44-750]
Ligand
BDBM17758
Substrate
BDBM17658
Meas. Tech.
Microplate GCPII Radioactivity-Based Assay
pH
7.4±n/a
Temperature
310.15±n/a K
IC50
30±n/a 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:
BDBM17758
Synonyms:
(2R)-2-(phosphonomethyl)pentanedioic acid | (R)-2-PMPA | pentanedioic acid analogue, (R)-1
Type:
Small organic molecule
Emp. Form.:
C6H11O7P
Mol. Mass.:
226.1211
SMILES:
OC(=O)CC[C@@H](CP(O)(O)=O)C(O)=O |r|