vipivotide tetraxetan [Ligand Id: 11982] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4594280 (DKFZ-PSMA-617, PSMA-617, PSMA617, Vipivotida tetraxetan, Vipivotide tetraxetan)
  • Folate hydrolase (prostate-specific membrane antigen) 1/Glutamate carboxypeptidase II in Human [ChEMBL: CHEMBL1892] [GtoPdb: 1606] [UniProtKB: Q04609]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Folate hydrolase (prostate-specific membrane antigen) 1/Glutamate carboxypeptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1892] [GtoPdb: 1606] [UniProtKB: Q04609]
ChEMBL Binding affinity to PSMA in human LNCaP cells after 45 mins in presence of 68Ga-labeled PSMA-10 by gamma counting assay B 8.63 pKi 2.34 nM Ki J Med Chem (2016) 59: 1761-1775 [PMID:26878194]
GtoPdb Inhibition of PSMA enzymatic activity - 9.43 pKi 0.37 nM Ki J Nucl Med (2015) 56: 914-20 [PMID:25883127]
ChEMBL Displacement of [125I]MIP-1095 from PSMA in human PC3-PIP cells after 1 hr by gamma counter analysis B 7.96 pIC50 10.9 nM IC50 Bioorg Med Chem (2020) 28: 115319-115319 [PMID:32001090]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]