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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 |
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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 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]