PBD150 [Ligand Id: 8356] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL201747
  • glutaminyl-peptide cyclotransferase/Glutaminyl-peptide cyclotransferase in Human [ChEMBL: CHEMBL4508] [GtoPdb: 2411] [UniProtKB: Q16769]
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  • glutaminyl-peptide cyclotransferase like/Glutaminyl-peptide cyclotransferase-like protein in Human [ChEMBL: CHEMBL3638349] [GtoPdb: 3289] [UniProtKB: Q9NXS2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
glutaminyl-peptide cyclotransferase/Glutaminyl-peptide cyclotransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4508] [GtoPdb: 2411] [UniProtKB: Q16769]
GtoPdb - - 7.22 pKi 60 nM Ki J Med Chem (2006) 49: 664-77 [PMID:16420052]
ChEMBL Inhibitory activity against human glutaminyl cyclase B 7.22 pKi 60 nM Ki J Med Chem (2006) 49: 664-677 [PMID:16420052]
ChEMBL Inhibition of human glutaminyl cyclase expressed in Pichia pastoris by pGAP coupled enzyme assay B 7.22 pKi 60 nM Ki J Med Chem (2009) 52: 7069-7080 [PMID:19863057]
ChEMBL Inhibition of human recombinant glutaminyl cyclase expressed in Escherichia coli using H-Gln-Gln-H substrate measured for 15 mins by spectrophotometry B 5.28 pIC50 5300 nM IC50 Bioorg Med Chem (2016) 24: 2280-2286 [PMID:27061673]
ChEMBL Inhibition of recombinant human QC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis B 7.54 pIC50 29 nM IC50 ACS Med Chem Lett (2022) 13: 1459-1467 [PMID:36105338]
glutaminyl-peptide cyclotransferase like/Glutaminyl-peptide cyclotransferase-like protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638349] [GtoPdb: 3289] [UniProtKB: Q9NXS2]
ChEMBL Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis B 6.45 pIC50 351 nM IC50 ACS Med Chem Lett (2022) 13: 1459-1467 [PMID:36105338]

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]