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ChEMBL ligand: CHEMBL1639 (Aliskiren, Rasilez, SPP-100, SPP100) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 renin activity in human plasma by competitive radio immunoassay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1351-1357 [PMID:35978678] |
ChEMBL | Inhibition of human plasma renin | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2022) 65: 10882-10897 [PMID:35939295] |
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 recombinant glycosylated human renin expressed in CHO cells | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2022) 65: 10882-10897 [PMID:35939295] |
ChEMBL | Inhibition of human recombinant renin using Nma-Lys-His-Pro-Phe-His-Leu-Val-Ile-His-Lys-Dnp substrate incubated for 1 hr by FRET | B | 9.15 | pIC50 | 0.7 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1351-1357 [PMID:35978678] |
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 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 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 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 human renin | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Eur J Med Chem (2011) 46: 2469-2476 [PMID:21497958] |
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 renin (unknown origin) | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1592-1596 [PMID:25728416] |
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 | B | 9.22 | pIC50 | 0.6 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1351-1357 [PMID:35978678] |
ChEMBL | Inhibition of renin activity in human plasma | B | 9.22 | pIC50 | 0.6 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1351-1357 [PMID:35978678] |
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 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]