phosphoramidon [Ligand Id: 11653] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL479579 (Phosphoramidon, Phosphramidon, Phosporamidon) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| 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 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]
