compound 35 [PMID: 24157366] [Ligand Id: 8554] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3086040
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  • Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Human [ChEMBL: CHEMBL2335] [GtoPdb: 1584] [UniProtKB: P42785]
  • Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Mouse [ChEMBL: CHEMBL1255149] [GtoPdb: 1584] [UniProtKB: Q7TMR0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 6.23 pIC50 590 nM IC50 Bioorg Med Chem Lett (2013) 23: 6228-6233 [PMID:24157366]
Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2335] [GtoPdb: 1584] [UniProtKB: P42785]
ChEMBL Enzyme Activity Assay: The potency of compounds of formula I against PrCP was determined by a fluorescence intensity kinetic assay measuring the IC50 values of PrCP inhibitor test compounds. Recombinant human and mouse PrCP enzymes from CHO or HEK expression systems (with comparable results for HEK enzymes) were prepared in-house and used in the assay. The assay was run on a Perkin Elmer Envision 2103 plate reader using a 320 nm excitation filter and a 405 emission filter. The assay was performed using a Hamilton Star liquid handling workstation. The assay employed the internally quenched fluorescent substrate (1S)-1-carboxy-5-[(2,4-dinitrophenyl)amino]pentyl N-[(7-methoxy-2-oxo-2H-chromen-4-yl)acetyl]-L-alanyl-L-prolinate prepared in house. B 9.8 pIC50 0.16 nM IC50 US-8669252-B2. Prolylcarboxypeptidase inhibitors (2014)
GtoPdb - - 10.1 pIC50 0.08 nM IC50 Bioorg Med Chem Lett (2013) 23: 6228-33 [PMID:24157366]
ChEMBL Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assay B 10.1 pIC50 0.08 nM IC50 Bioorg Med Chem Lett (2013) 23: 6228-6233 [PMID:24157366]
Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255149] [GtoPdb: 1584] [UniProtKB: Q7TMR0]
ChEMBL Inhibition of recombinant mouse PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assay B 9.55 pIC50 0.28 nM IC50 Bioorg Med Chem Lett (2013) 23: 6228-6233 [PMID:24157366]

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]