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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]