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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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 data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]