sacubitrilat [Ligand Id: 7858] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL417007 (Lbq-657)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Angiotensin-converting enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821]
ChEMBL Inhibition of human ACE using MCA-RPPGFSAFK-Dnp-OH as substrate by fluorescence based analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2020) 63: 5488-5500 [PMID:32337993]
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Inhibition of human NEP using MCA-RPPGFSAFK-Dnp-OH as substrate by fluorescence based analysis B 7.7 pIC50 20 nM IC50 J Med Chem (2020) 63: 5488-5500 [PMID:32337993]
GtoPdb - - 8.14 pIC50 7.3 nM IC50 Inhibition of the renin - angiotensin system – present and future challenges.. Heart Failure Update 2014
ChEMBL Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured after 1 hr by fluorescence based assay B 8.22 pIC50 6 nM IC50 ACS Med Chem Lett (2020) 11: 188-194 [PMID:32071687]
Neutral endopeptidase/Neprilysin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3369] [GtoPdb: 1611] [UniProtKB: P07861]
ChEMBL In vitro inhibition of rat neutral endopeptidase by using GAAP as substrate B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1995) 38: 1689-1700 [PMID:7752193]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]