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]
Created with Highcharts 10.3.3ValuesChart context menuCystinyl aminopeptidasepKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Endoplasmic reticulum aminopeptidase 1 in Human [ChEMBL: CHEMBL5939] [GtoPdb: 1566] [UniProtKB: Q9NZ08]
Created with Highcharts 10.3.3ValuesChart context menuEndoplasmic reticulum aminopeptidase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Endoplasmic reticulum aminopeptidase 2 in Human [ChEMBL: CHEMBL5043] [GtoPdb: 1567] [UniProtKB: Q6P179]
Created with Highcharts 10.3.3ValuesChart context menuEndoplasmic reticulum aminopeptidase 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
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 35:

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]