kelatorphan [Ligand Id: 11656] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL85320 (Kelatorphan) |
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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 | Compound was evaluated for inhibition of enkephalin degrading enzyme, aminopeptidase N(APN) | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (2001) 44: 3523-3530 [PMID:11585456] |
| Aminopeptidase N in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2590] [UniProtKB: P15145] | ||||||||
| ChEMBL | Inhibitory activity against aminopeptidase using 10 nM of [3H]Leu-enkephalin as substrate | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1985) 28: 1158-1169 [PMID:3897541] |
| Angiotensin-converting enzyme in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4074] [UniProtKB: P12822] | ||||||||
| ChEMBL | Inhibitory activity against rabbit lung angiotensin-converting enzyme (ACE) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2517-2522 |
| Endothelin-converting enzyme 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4791] [GtoPdb: 1615] [UniProtKB: P42892] | ||||||||
| ChEMBL | Inhibitory activity against human bronchiolar smooth muscle Endothelin-converting enzyme 1 | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960] | ||||||||
| ChEMBL | Inhibitory activity against LTA 4 hydrolase in epoxide hydrolase assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2517-2522 |
| GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | Bioorganic and Medicinal Chemistry Letters (1995) 5: 2517-2522 |
| ChEMBL | Inhibitory activity against LTA 4 hydrolase in aminopeptidase assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2517-2522 |
| ChEMBL | Inhibitory activity was determined for LTB4 production in human whole blood. | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2000) 43: 721-735 [PMID:10691697] |
| ChEMBL | Inhibitory activity against recombinant human Leukotriene A4 hydrolase | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2517-2522 |
| ChEMBL | Inhibitory activity was determined against Leukotriene A4 hydrolase | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2000) 43: 721-735 [PMID:10691697] |
| Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473] | ||||||||
| ChEMBL | Compound was evaluated for inhibition of enkephalin degrading enzyme, neutral endopeptidase (NEP) | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2001) 44: 3523-3530 [PMID:11585456] |
| GtoPdb | - | - | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2001) 44: 3523-30 [PMID:11585456] |
| Neprilysin in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3768] [UniProtKB: P08049] | ||||||||
| ChEMBL | Inhibitory activity against rabbit kidney neutral endopeptidase (NEP) | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2517-2522 |
| ChEMBL | Inhibitory activity against big ET-1 of Neutral endopeptidase | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| ChEMBL | Inhibition of [3H]Ala2-Leu-enkephalin binding to Neutral endopeptidase (NEP) | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (1988) 31: 1825-1831 [PMID:2900898] |
| ChEMBL | Inhibitory activity against Leu-enkeph of Neutral endopeptidase | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| Neutral endopeptidase/Neprilysin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3369] [GtoPdb: 1611] [UniProtKB: P07861] | ||||||||
| ChEMBL | 50% inhibitory activity against enkephalinase purified from rat kidney with [3H]D-Ala2-Leu-enkephalin (20 nM) as substrate. | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (1985) 28: 1158-1169 [PMID:3897541] |
| Thermolysin in Bacillus thermoproteolyticus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3392] [UniProtKB: P00800] | ||||||||
| ChEMBL | Inhibitory activity against thermolysin with 0.5 uM [Leu5]-enkephalin (NEN) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
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]
