kelatorphan [Ligand Id: 11656] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL85320 (Kelatorphan)
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  • Angiotensin-converting enzyme in Rabbit [ChEMBL: CHEMBL4074] [UniProtKB: P12822]
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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
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  • Thermolysin in Bacillus thermoproteolyticus [ChEMBL: CHEMBL3392] [UniProtKB: P00800]
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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 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]