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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
