compound 17 [PMID: 23916253] [Ligand Id: 8666] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2420382
  • Leucyl-cysteinyl aminopeptidase/Cystinyl aminopeptidase in Human [ChEMBL: CHEMBL2693] [GtoPdb: 1570] [UniProtKB: Q9UIQ6]
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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
Leucyl-cysteinyl aminopeptidase/Cystinyl aminopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2693] [GtoPdb: 1570] [UniProtKB: Q9UIQ6]
GtoPdb - - 5.22 pIC50 6000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-6 [PMID:23916253]
ChEMBL Inhibition of human recombinant IRAP expressed in HeLa cells assessed as L-Leucine-7-amido-4-methyl coumarin hydrolysis to 7-amido-4-methyl coumarin after 5 to 10 mins by fluorescence assay B 5.22 pIC50 6000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-4836 [PMID:23916253]
Endoplasmic reticulum aminopeptidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5939] [GtoPdb: 1566] [UniProtKB: Q9NZ08]
ChEMBL Inhibition of recombinant ERAP1 (unknown origin) expressed in baculovirus-infected Hi5 insect cells assessed as L-Leucine-7-amido-4-methyl coumarin hydrolysis to 7-amido-4-methyl coumarin after 5 to 10 mins by fluorescence assay B 5.59 pIC50 2600 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-4836 [PMID:23916253]
GtoPdb - - 5.59 pIC50 2600 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-6 [PMID:23916253]
Endoplasmic reticulum aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5043] [GtoPdb: 1567] [UniProtKB: Q6P179]
GtoPdb - - 5.05 pIC50 8900 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-6 [PMID:23916253]
ChEMBL Inhibition of recombinant ERAP2 (unknown origin) expressed in baculovirus-infected Hi5 insect cells assessed as L-Arginyl-7-amido-4-methyl coumarin hydrolysis to 7-amido-4-methyl coumarin after 5 to 10 mins by fluorescence assay B 5.05 pIC50 8900 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4832-4836 [PMID:23916253]

ChEMBL data shown on this page come from version 26:

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]