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

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ChEMBL ligand: CHEMBL298827
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  • Thermolysin in Bacillus thermoproteolyticus [ChEMBL: CHEMBL3392] [UniProtKB: P00800]
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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 recombinant human Aminopeptidase N using L-Ala-beta-NA as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorometry B 5 pKi >10000 nM Ki Eur J Med Chem (2015) 102: 58-67 [PMID:26241877]
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 4.99 pIC50 10200 nM IC50 J Med Chem (2020) 63: 5488-5500 [PMID:32337993]
ChEMBL Inhibitory activity against angiotensin I converting enzyme (ACE) B 6.07 pIC50 860 nM IC50 J Med Chem (2000) 43: 305-341 [PMID:10669559]
ChEMBL Inhibitory activity against angiotensin-converting enzyme (ACE). B 6.85 pIC50 140 nM IC50 J Med Chem (2000) 43: 305-341 [PMID:10669559]
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Inhibition of recombinant human Neprilysin using Suc-Ala-Ala-Phe-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorometry B 8.26 pKi 5.5 nM Ki Eur J Med Chem (2015) 102: 58-67 [PMID:26241877]
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 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]
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]
Neprilysin in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3768] [UniProtKB: P08049]
ChEMBL Tested for binding affinity against neutral endopeptidase (NEP) B 8.72 pKi 1.9 nM Ki J Med Chem (1994) 37: 1865-1873 [PMID:8021926]
ChEMBL Tested for inhibition against neutral endopeptidase (NEP) B 8.72 pIC50 1.9 nM IC50 J Med Chem (1994) 37: 1865-1873 [PMID:8021926]
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 Inhibitory activity against Endopeptidase B 8.4 pIC50 4 nM IC50 J Med Chem (2000) 43: 305-341 [PMID:10669559]
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]
Thermolysin in Bacillus thermoproteolyticus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3392] [UniProtKB: P00800]
ChEMBL Tested for binding against Thermolysin B 5.74 pKi 1800 nM Ki J Med Chem (1994) 37: 1865-1873 [PMID:8021926]
ChEMBL Tested for binding affinity against Thermolysin B 5.74 pIC50 1800 nM IC50 J Med Chem (1994) 37: 1865-1873 [PMID:8021926]

ChEMBL data shown on this page come from version 32:

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]