compound I3 [PMID: 23428964] [Ligand Id: 8565] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1852660
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  • Endoplasmic reticulum aminopeptidase 1 in Human [ChEMBL: CHEMBL5939] [GtoPdb: 1566] [UniProtKB: Q9NZ08]
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  • Endoplasmic reticulum aminopeptidase 2 in Human [ChEMBL: CHEMBL5043] [GtoPdb: 1567] [UniProtKB: Q6P179]
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  • Interleukin-1 receptor antagonist protein in Human [ChEMBL: CHEMBL4523191] [UniProtKB: P18510]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aminopeptidase N in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1907] [GtoPdb: 1560] [UniProtKB: P15144]
ChEMBL Inhibition of human APN using L-leucine-p-nitroanilide as substrate measured every 10 mins for 2 hrs by spectrophotometric analysis B 9.46 pKi 0.35 nM Ki Bioorg Med Chem (2013) 21: 2135-2144 [PMID:23428964]
GtoPdb - - 9.46 pKi 0.35 nM Ki Bioorg Med Chem (2013) 21: 2135-44 [PMID:23428964]
Aminopeptidase N in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2590] [UniProtKB: P15145]
ChEMBL Inhibition of pig APN using L-leucine-p-nitroanilide as substrate measured every 10 mins for 2 hrs by spectrophotometric analysis B 10.22 pKi 0.06 nM Ki Bioorg Med Chem (2013) 21: 2135-2144 [PMID:23428964]
Aminopeptidase N in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189140] [GtoPdb: 1560] [UniProtKB: P97449]
ChEMBL Inhibition of mouse APN using L-leucine-p-nitroanilide as substrate measured every 10 mins for 2 hrs by spectrophotometric analysis B 9.7 pKi 0.2 nM Ki Bioorg Med Chem (2013) 21: 2135-2144 [PMID:23428964]
GtoPdb - - 9.7 pKi 0.2 nM Ki Bioorg Med Chem (2013) 21: 2135-44 [PMID:23428964]
Endoplasmic reticulum aminopeptidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5939] [GtoPdb: 1566] [UniProtKB: Q9NZ08]
ChEMBL Inhibition of human recombinant ERAP1 expressed in baculovirus infected sf9 cells using L-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis B 5.8 pIC50 1600 nM IC50 J Med Chem (2024) 67: 11597-11621 [PMID:39011823]
Endoplasmic reticulum aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5043] [GtoPdb: 1567] [UniProtKB: Q6P179]
ChEMBL Inhibition of human recombinant ERAP2 expressed in baculovirus infected sf9 cells using R-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis B 6.41 pIC50 390 nM IC50 J Med Chem (2024) 67: 11597-11621 [PMID:39011823]
Interleukin-1 receptor antagonist protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523191] [UniProtKB: P18510]
ChEMBL Inhibition of human recombinant IRAP expressed in baculovirus infected Sf9 cells using L-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis B 6.92 pIC50 120 nM IC50 J Med Chem (2024) 67: 11597-11621 [PMID:39011823]

ChEMBL data shown on this page come from version 36:

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]