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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, P; Hin, B; Stoermer, D; Adams, J; Xu, W; Duvall, BR; Delahanty, G; Liu, Q; Stathis, MJ; Wozniak, KM; Slusher, BS; Tsukamoto, 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
More Info.:
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