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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
