aliskiren [Ligand Id: 4812] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1639 (Aliskiren, Rasilez, SPP100, SPP-100)
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]