opiorphin [Ligand Id: 11538] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2022225 (Opiorphin)
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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 AP-N ectopeptidase activity using alanine-MCA as substrate preincubated for 10 mins with substrate by fluorimetric analysis B 5.09 pIC50 8100 nM IC50 J. Med. Chem. (2012) 55: 1181-1188 [PMID:22224710]
ChEMBL Inhibition of human recombinant aminopeptidase N using AbzdR-G-L-EDDnp as substrate after 20 to 40 mins by fluorometry B 5.09 pIC50 8100 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5190-5193 [PMID:26463133]
ChEMBL Inhibition of human recombinant aminopeptidase N using Ala-Mca as substrate incubated for 10 mins prior to substrate addition measured for 40 mins by fluorometry B 5.1 pIC50 8000 nM IC50 ACS Med. Chem. Lett. (2012) 3: 20-24 [PMID:24900367]
GtoPdb - - 5.1 pIC50 8000 nM IC50 ACS Med Chem Lett (2012) 3: 20-4 [PMID:24900367]
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Inhibition of human recombinant NEP ectopeptidase activity using Abz-dRGL-(EDDnp) as substrate preincubated for 10 mins with substrate by fluorimetric analysis B 4.52 pIC50 30000 nM IC50 J. Med. Chem. (2012) 55: 1181-1188 [PMID:22224710]
ChEMBL Inhibition of human recombinant neprilysin using Abz-dR-G-L-EDDnp as substrate incubated for 10 mins prior to substrate addition measured for 40 mins by fluorometry B 4.52 pIC50 30000 nM IC50 ACS Med. Chem. Lett. (2012) 3: 20-24 [PMID:24900367]
ChEMBL Inhibition of human recombinant neutral endopeptidase using Ala-AMC as substrate after 20 to 40 mins by fluorometry B 4.52 pIC50 30000 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5190-5193 [PMID:26463133]

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]