compound 2g [PMID: 27390066] [Ligand Id: 9682] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3355101
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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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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 recombinant alanyl aminopeptidase after 30 to 60 mins by morrison's equation B 8.62 pKi 2.4 nM Ki J Med Chem (2014) 57: 8140-8151 [PMID:25192493]
Aminopeptidase N in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2590] [UniProtKB: P15145]
ChEMBL Inhibition of pig recombinant alanyl aminopeptidase after 30 to 60 mins by morrison's equation B 7.16 pKi 69 nM Ki J Med Chem (2014) 57: 8140-8151 [PMID:25192493]
Cytosol aminopeptidase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5624] [UniProtKB: P28839]
ChEMBL Inhibition of pig recombinant leucine aminopeptidase after 30 to 60 mins by morrison's equation B 6.67 pKi 215 nM Ki J Med Chem (2014) 57: 8140-8151 [PMID:25192493]
Endoplasmic reticulum aminopeptidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5939] [GtoPdb: 1566] [UniProtKB: Q9NZ08]
ChEMBL Inhibition of human ERAP1 preincubated for 30 to 60 mins followed by addition of Leu-AMC as substrate measured for 15 mins by spectrofluorimetric method B 6.28 pKi 530 nM Ki Bioorg Med Chem Lett (2016) 26: 4122-4126 [PMID:27390066]
GtoPdb - - 6.28 pKi 530 nM Ki Bioorg Med Chem Lett (2016) 26: 4122-6 [PMID:27390066]
Endoplasmic reticulum aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5043] [GtoPdb: 1567] [UniProtKB: Q6P179]
ChEMBL Inhibition of human ERAP2 preincubated for 30 to 60 mins followed by addition of Arg-AMC as substrate measured for 15 mins by spectrofluorimetric method B 6.82 pKi 152 nM Ki Bioorg Med Chem Lett (2016) 26: 4122-4126 [PMID:27390066]
GtoPdb - - 6.82 pKi 150 nM Ki Bioorg Med Chem Lett (2016) 26: 4122-6 [PMID:27390066]

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]