phosphoramidon [Ligand Id: 11653] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL479579 (Phosphoramidon, Phosphramidon, Phosporamidon) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Endothelin-converting enzyme 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4791] [GtoPdb: 1615] [UniProtKB: P42892] | ||||||||
| ChEMBL | Inhibition of putative Endothelin-converting enzyme partially purified from rabbit lung membranes | B | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1953-1958 |
| ChEMBL | Inhibition of endothelin converting enzyme in an RIA assay using ET-1 as substrate (value corresponds to <25% inhibition when assayed at a 100 uM screening concentration) | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1993) 36: 173-176 [PMID:8421284] |
| ChEMBL | In Vitro inhibition of recombinant human endothelin converting enzyme-1 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2000) 43: 488-504 [PMID:10669576] |
| ChEMBL | In vitro inhibition against recombinant human Endothelin converting enzyme 1 activity | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 1059-1064 |
| ChEMBL | Inhibitory activity was assessed on CHO cells expressing recombinant human Endothelin-converting enzyme 1 (ECE-1). | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (1998) 41: 1513-1523 [PMID:9554884] |
| ChEMBL | Inhibition of human somatic ECE1 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2010) 53: 208-220 [PMID:19899765] |
| ChEMBL | Inhibitory concentration against human ECE-1 by RIA | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (2005) 48: 483-498 [PMID:15658862] |
| ChEMBL | Inhibition of endothelin-converting enzyme in human umbilical vein endothelial cells | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1323-1326 |
| ChEMBL | In vitro inhibition of phosphoramidon-sensitive membrane bound zinc metalloprotease Endothelin-converting enzyme from partially purified guinea pig lungs | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1629-1634 |
| ChEMBL | Inhibition of Endothelin-converting enzyme of guinea pig lung membrane | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1257-1260 |
| ChEMBL | Inhibition of human recombinant ECE1 by fluorimetry | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4715-4719 [PMID:19596577] |
| ChEMBL | Inhibitory activity against human bronchiolar smooth muscle Endothelin-converting enzyme 1 | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| Endothelin-converting enzyme 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2340] [UniProtKB: P42891] | ||||||||
| ChEMBL | Inhibition of Endothelin-converting enzyme (ECE) from microsomal fractions of bovine cultured endothelial cells | B | 5.51 | pIC50 | 3100 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1257-1262 |
| Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473] | ||||||||
| ChEMBL | Inhibitory activity against neutral endopeptidase (NEP) from human blood serum | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2003) 46: 3326-3332 [PMID:12852763] |
| ChEMBL | Inhibition of neutral endopeptidase 24.11(NEP) | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 1059-1064 |
| ChEMBL | Inhibitory activity against neutral endopeptidase (NEP). | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1998) 41: 1513-1523 [PMID:9554884] |
| ChEMBL | Inhibition of human somatic NEP | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 208-220 [PMID:19899765] |
| ChEMBL | Inhibition of neutral endopeptidase in human fibroblasts homogenates using glutaryl-Ala-Ala-Phe-4-methoxy-2-naphtylamide as substrate after 1 hrs by fluorimetric assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2011) 19: 5935-5947 [PMID:21937235] |
| Neprilysin in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3768] [UniProtKB: P08049] | ||||||||
| ChEMBL | Inhibitory activity against Leu-enkeph of Neutral endopeptidase | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| ChEMBL | Inhibitory activity against big ET-1 of Neutral endopeptidase | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1995) 38: 2119-2129 [PMID:7783143] |
| ChEMBL | Inhibition of enkephalinase activity in membranes prepared from rabbit | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (1989) 32: 2519-2526 [PMID:2585440] |
| Neutral endopeptidase/Neprilysin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3369] [GtoPdb: 1611] [UniProtKB: P07861] | ||||||||
| ChEMBL | Binding affinity towards enkephalinase (metalloendopeptidase, E.C.3.4.24.11) of rat kidney | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1985) 28: 1208-1216 [PMID:2993614] |
| GtoPdb | Inhibition of enkephalinase from rat kidney | - | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1985) 28: 1208-16 [PMID:2993614] |
| ChEMBL | Inhibitory activity against neutral endopeptidase (NEP) from rat cortex brain membrane | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2003) 46: 3326-3332 [PMID:12852763] |
| ChEMBL | Inhibition of rat kidney NEP using glutaryl-Ala-Ala-beta-naphthylamide as substrate preincubated with enzyme for 15 mins followed by substrate addition | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2020) 63: 5488-5500 [PMID:32337993] |
| ChEMBL | In vitro inhibition of rat neutral endopeptidase | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2000) 43: 488-504 [PMID:10669576] |
| ChEMBL | In vitro inhibition of Neutral endopeptidase (NEP) enzyme | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1994) 37: 498-511 [PMID:8120868] |
| ChEMBL | Evaluation of in vitro inhibitory activity against Neutral endopeptidase | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (1995) 38: 5023-5030 [PMID:8544178] |
| ChEMBL | compound was tested for inhibitory activity against neutral endopeptidase (NEP) | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1257-1260 |
| ChEMBL | Inhibitory activity against neutral endopeptidase (NEP)prepared from microsomal fractions of rat small intestine | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1257-1262 |
| ChEMBL | Inhibition of enkephalinase activity in synaptic membranes prepared from rat striatum | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (1989) 32: 2519-2526 [PMID:2585440] |
| Pseudolysin in Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075146] [UniProtKB: P14756] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa LasB elastase using aminobenzoyl-Ala-Gly-Leu-Ala-p-nitro-benzyl-amide as substrate b microtiter-based fluorimetric assay | B | 7.24 | pKi | 57 | nM | Ki | J Med Chem (2016) 59: 5929-5969 [PMID:26804741] |
| Thermolysin in Bacillus thermoproteolyticus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3392] [UniProtKB: P00800] | ||||||||
| ChEMBL | Binding affinity against Thermolysin | B | 7.56 | pKd | -7.56 | - | Log Kd | J Med Chem (2002) 45: 2770-2780 [PMID:12061879] |
| ChEMBL | Inhibitory constant against thermolysin. | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (1992) 35: 1671-1684 [PMID:1588550] |
| ChEMBL | Inhibitory activity against thermolysin with 0.5 uM [Leu5]-enkephalin (NEN) | B | 7.48 | pIC50 | 33 | 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]
