sacubitrilat [Ligand Id: 7858] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL417007 (Lbq-657, LBQ657, Sacubitrilat) |
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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 34:
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]
