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: CHEMBL1639 (Aliskiren, Rasilez, SPP100, SPP-100) |
---|
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 |
---|---|---|---|---|---|---|---|---|
Cathepsin D in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4106] [UniProtKB: P80209] | ||||||||
ChEMBL | Inhibition of bovine cathepsin D | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4863-4867 [PMID:19615901] |
Protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366517] [UniProtKB: Q9YQ12] | ||||||||
ChEMBL | Inhibition of HIV1 recombinant protease using Lys-Ala-Arg-Val-Nle-Nph-Glu-Ala-Nle-NH2 as substrate by spectrophotometric analysis | B | 7.12 | pKi | 76.5 | nM | Ki | J Med Chem (2012) 55: 5784-5796 [PMID:22621689] |
Renin in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287631] [UniProtKB: Q6DLW5] | ||||||||
ChEMBL | Inhibition of renin in monkey plasma | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem (2018) 26: 3261-3286 [PMID:29754833] |
renin/Renin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL286] [GtoPdb: 2413] [UniProtKB: P00797] | ||||||||
ChEMBL | Inhibition of recombinant human renin using 5-FAM/QXL 520 as substrate pretreated for 30 mins followed by substrate addition measured at 1 min interval for 15 mins by FRET assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2017) 25: 3947-3963 [PMID:28601508] |
ChEMBL | Inhibition of human recombinant renin preincubated for 30 mins followed by substrate addition measured after 15 mins by fluorescence analysis | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2015) 103: 269-288 [PMID:26363506] |
ChEMBL | Inhibition of renin measured every 30 secs for 15 mins by fluorimetric analysis | B | 8.66 | pIC50 | 2.21 | nM | IC50 | Bioorg Med Chem (2011) 19: 4238-4249 [PMID:21708467] |
ChEMBL | Inhibition of renin in human plasma by radioimmunoassay | B | 9.08 | pIC50 | 0.84 | nM | IC50 | Bioorg Med Chem (2018) 26: 3261-3286 [PMID:29754833] |
ChEMBL | Inhibition of human recombinant renin assessed as decrease in plasma renin activity by competitive radioimmunoassay in presence of human plasma | B | 9.19 | pIC50 | 0.65 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 694-699 [PMID:19959358] |
ChEMBL | Inhibition of renin in human plasma assessed as formation of angiotensin1 product after 90 mins by competitive radioimmunoassay | B | 9.19 | pIC50 | 0.65 | nM | IC50 | ACS Med Chem Lett (2011) 2: 747-751 [PMID:24900262] |
GtoPdb | - | - | 9.2 | pIC50 | 0.6 | nM | IC50 | Clin Exp Pharmacol Physiol (2008) 35: 426-30 [PMID:18307734] |
ChEMBL | Inhibition of human renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Eur J Med Chem (2011) 46: 2469-2476 [PMID:21497958] |
ChEMBL | Inhibition of purified recombinant human renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4863-4867 [PMID:19615901] |
ChEMBL | Inhibition of human plasma renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4863-4867 [PMID:19615901] |
ChEMBL | Inhibition of renin in plasma | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2010) 53: 7490-7520 [PMID:20731374] |
ChEMBL | Inhibition of renin (unknown origin) | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1592-1596 [PMID:25728416] |
ChEMBL | Inhibition of human recombinant rennin in buffer assessed as accumulation of angiotensin 1 using human tetradecapeptide by immunoassay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2009) 52: 3689-3702 [PMID:19358611] |
ChEMBL | Inhibition of recombinant human renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2017) 25: 3947-3963 [PMID:28601508] |
ChEMBL | Inhibition of human recombinant renin in presence of human plasma by competitive radioimmunoassay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3541-3545 [PMID:19457666] |
ChEMBL | Inhibition of human renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2012) 55: 5784-5796 [PMID:22621689] |
ChEMBL | Inhibition of trypsin-activated human recombinant renin | B | 9.28 | pIC50 | 0.53 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 694-699 [PMID:19959358] |
ChEMBL | Inhibition of human recombinant renin using H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Asn-OH as substrate assessed as formation of angiotensin1 product after 2 hrs by competive radioimmunoassay | B | 9.28 | pIC50 | 0.53 | nM | IC50 | ACS Med Chem Lett (2011) 2: 747-751 [PMID:24900262] |
ChEMBL | Inhibition of human recombinant renin | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3541-3545 [PMID:19457666] |
ChEMBL | Inhibition of human recombinant renin using DABCYL-gamma-Abu-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS as substrate for 60 mins by fluorimetry | B | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 747-751 [PMID:24900262] |
Renin in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287632] [UniProtKB: Q7M3D2] | ||||||||
ChEMBL | Inhibition of rabbit renin | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2010) 53: 7490-7520 [PMID:20731374] |
renin/Renin in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2615] [GtoPdb: 2413] [UniProtKB: P06281] | ||||||||
ChEMBL | Inhibition of mouse renin | B | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2010) 53: 7490-7520 [PMID:20731374] |
renin/Renin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2322] [GtoPdb: 2413] [UniProtKB: P08424] | ||||||||
ChEMBL | Inhibition of renin in rat plasma | B | 7.06 | pIC50 | 88 | nM | IC50 | Bioorg Med Chem (2018) 26: 3261-3286 [PMID:29754833] |
ChEMBL | Inhibition of rat renin | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2010) 53: 7490-7520 [PMID:20731374] |
ChEMBL data shown on this page come from version 32:
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]