thiorphan [Ligand Id: 5278] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL298827
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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 Binding affinity to angiotensin-converting enzyme (unknown origin) assessed as inhibition constant B 6.89 pKi 130 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Compound was evaluated for inhibition of recombinant human neprilysin(NEP). B 8.66 pKi 2.2 nM Ki Bioorg Med Chem Lett (1996) 6: 2437-2440
ChEMBL Binding affinity to neutral endopeptidase (unknown origin) assessed as inhibition constant B 8.72 pKi 1.9 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
ChEMBL Inhibition of human recombinant NEP using Suc-Ala-Ala-Phe-AMC as substrate after 30 mins by fluorimetry B 8.82 pKi 1.5 nM Ki J Med Chem (2014) 57: 5748-5763 [PMID:24927250]
Neutral endopeptidase/Neprilysin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3369] [GtoPdb: 1611] [UniProtKB: P07861]
ChEMBL Inhibition of neutral endopeptidase (NEP). B 8.72 pKi 1.9 nM Ki Bioorg Med Chem Lett (1996) 6: 2053-2058
ChEMBL Compound was tested for inhibition of rat kidney neutral endopeptidase B 8.72 pIC50 1.9 nM IC50 Bioorg Med Chem Lett (1996) 6: 2097-2102
ChEMBL Concentration for 50% inhibition of activity of rat kidney enkephalinase F 8.72 pIC50 1.9 nM IC50 J Med Chem (1986) 29: 751-757 [PMID:3517331]

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]