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 | 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] |
| 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 | 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] |
| 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 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]
