enalaprilat [Ligand Id: 6332] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL577 (Enalaprilat anhydrous, MK-421) |
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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 | In vitro inhibitory activity against Angiotensin I converting enzyme from unpurified guinea pig serum | B | 5.51 | pIC50 | 3100 | nM | IC50 | J Med Chem (1985) 28: 1291-1295 [PMID:2993618] |
| GtoPdb | - | - | 7.5 | pIC50 | 34 | nM | IC50 | J Cardiovasc Pharmacol (1994) 23 Suppl 4: S11-5 [PMID:7527095] |
| ChEMBL | Inhibition of angiotensin I converting enzyme in silico | B | 8.4 | pIC50 | 3.98 | nM | IC50 | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
| ChEMBL | Compound was tested for its inhibitory potency against angiotensin I converting enzyme. | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1991) 34: 511-517 [PMID:1995872] |
| ChEMBL | Inhibition of Angiotensin I converting enzyme from pig renal cortex, hippuryl-histidyl-leucine as substrate | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (1989) 32: 289-297 [PMID:2913292] |
| ChEMBL | Compound tested in vitro for inhibition of Angiotensin I converting enzyme | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (1989) 32: 1600-1606 [PMID:2544729] |
| ChEMBL | Inhibition of human plasma ACE | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of guinea pig angiotensin I converting enzyme | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1986) 29: 1953-1961 [PMID:3020249] |
| ChEMBL | Inhibition of angiotensin-converting enzyme (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2016) 59: 10865-10890 [PMID:27690430] |
| ChEMBL | In vitro inhibitory activity against Angiotensin I converting enzyme | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1985) 28: 434-442 [PMID:2984419] |
| ChEMBL | Inhibitory concentration against Angiotensin I converting enzyme | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1986) 29: 251-260 [PMID:3005569] |
| ChEMBL | In vitro inhibition of Angiotensin I converting enzyme in Hog plasma | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1990) 33: 1606-1615 [PMID:2160536] |
| ChEMBL | Inhibition of Angiotensin I converting enzyme (ACE) in Bothrops jararaca venom | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2002) 45: 5609-5616 [PMID:12477342] |
| ChEMBL | Inhibition of Angiotensin I converting enzyme | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1993) 36: 2051-2058 [PMID:8340909] |
| Angiotensin-converting enzyme in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4074] [UniProtKB: P12822] | ||||||||
| ChEMBL | Inhibitory activity against rabbit lung angiotensin-1 converting enzyme | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1988) 31: 1148-1160 [PMID:2836590] |
| ChEMBL | Evaluation of in vitro inhibitory activity against Angiotensin I converting enzyme | B | 8.06 | pIC50 | 8.8 | nM | IC50 | J Med Chem (1995) 38: 5023-5030 [PMID:8544178] |
| ChEMBL | In vitro inhibition of Angiotensin I converting enzyme in rabbit lung | B | 8.24 | pIC50 | 5.8 | nM | IC50 | J Med Chem (1990) 33: 1606-1615 [PMID:2160536] |
| ChEMBL | Inhibitory activity against rabbit lung Angiotensin I converting enzyme with 5 mM hippuryl-histidyl-leucine as substrate | B | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (1987) 30: 1984-1991 [PMID:3669006] |
| ChEMBL | Concentration required for 50% inhibition of rabbit lung Angiotensin I converting enzyme with 5 mM hippuryl-histidyl-leucine as substrate | B | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (1988) 31: 422-428 [PMID:3339612] |
| ChEMBL | In vitro inhibition of angiotensin I converting enzyme in rabbit lung with hippuryl-histidyl-leucine as substrate | B | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (1988) 31: 204-212 [PMID:3336020] |
| ChEMBL | In vitro activity against angiotensin I converting enzyme especially against Hip-His-Leu residues | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1991) 34: 663-669 [PMID:1995891] |
| Angiotensin-converting enzyme in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2994] [GtoPdb: 1613] [UniProtKB: P09470] | ||||||||
| ChEMBL | Inhibition of ob/ob mouse plasma ACE | B | 7.94 | pIC50 | 11.5 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| Angiotensin-converting enzyme in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2625] [GtoPdb: 1613] [UniProtKB: P47820] | ||||||||
| ChEMBL | Inhibition of Wistar rat plasma ACE | B | 8.02 | pIC50 | 9.6 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | In vitro inhibitory activity against angiotensin I converting enzyme of rats. | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1988) 31: 1148-1160 [PMID:2836590] |
| ChEMBL | Inhibition of rat Angiotensin I converting enzyme (ACE), using Hip-Gly-Gly as synthetic substrate. | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (1987) 30: 992-998 [PMID:3035180] |
| ChEMBL | Compound was tested for inhibitory activity against angiotensin I converting enzyme | B | 9.02 | pIC50 | 0.95 | nM | IC50 | J Med Chem (1991) 34: 439-447 [PMID:1992145] |
| Angiotensin-converting enzyme 2/Angiotensin-converting enzyme-related carboxypeptidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2311] [GtoPdb: 1614] [UniProtKB: Q5EGZ1] | ||||||||
| ChEMBL | Binding affinity towards Angiotensin I converting enzyme of rat brain IgG immobilized enzyme. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1985) 28: 1208-1216 [PMID:2993614] |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487] | ||||||||
| ChEMBL | Inhibition of human plasma DPP4 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
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]
