tolrestat [Ligand Id: 7404] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL436 (Alderase, Alredase, AY-27773, AY-27,773, Tolrestat)
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  • Aldo-keto reductase family 1 member B10 in Human [ChEMBL: CHEMBL5983] [UniProtKB: O60218]
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  • aldo-keto reductase family 1 member B/Aldose reductase in Human [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
  • Aldose reductase in Pig [ChEMBL: CHEMBL4559] [UniProtKB: P80276]
  • Aldose reductase in Bovine [ChEMBL: CHEMBL3081] [UniProtKB: P16116]
  • aldo-keto reductase family 1 member B/Aldose reductase in Rat [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aldehyde reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2246] [UniProtKB: P14550]
ChEMBL In vitro inhibition of recombinant human aldehyde reductase B 5.71 pIC50 1940 nM IC50 J. Med. Chem. (2005) 48: 3141-3152 [PMID:15857120]
ChEMBL Inhibition of N-terminal 6His-tagged human aldehyde reductase expressed in Escherichia coli BL21(DE3) mediated D-glucuronate reduction B 6.14 pIC50 720 nM IC50 Bioorg. Med. Chem. (2010) 18: 2485-2490 [PMID:20304656]
Aldehyde reductase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4049] [UniProtKB: P50578]
ChEMBL Inhibition of pig ALR1 B 5.66 pIC50 2190 nM IC50 Bioorg. Med. Chem. (2009) 17: 1244-1250 [PMID:19121944]
ChEMBL Selectivity ratio measured as the IC50 ratio of aldehyde/aldose reductase values B 6.27 pIC50 540 nM IC50 J. Med. Chem. (1991) 34: 1011-1018 [PMID:1900532]
Aldehyde reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3871] [UniProtKB: P51635]
ChEMBL Evaluated for inhibition of Aldehyde reductase 1 B 5.92 pIC50 1210 nM IC50 J. Med. Chem. (1996) 39: 4396-4405 [PMID:8893834]
Aldo-keto reductase family 1 member B10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5983] [UniProtKB: O60218]
ChEMBL Inhibition of reductase activity of N-terminal 6His-tagged human AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as pyridine-3-aldehyde reduction B 7.3 pKi 50 nM Ki J. Nat. Prod. (2011) 74: 1201-1206 [PMID:21561086]
ChEMBL Inhibition of reductase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of NADPH linked pyridine-3-aldehyde reduction B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. (2010) 18: 2485-2490 [PMID:20304656]
ChEMBL Inhibition of human N-terminal His-tagged AKR1B10 expressed in Escherichia coli BL21 using retinaldehyde as substrate B 7.27 pIC50 54 nM IC50 J Med Chem (2017) 60: 8441-8455 [PMID:28976752]
ChEMBL Inhibition of retinaldehyde reductase activity of human AKR1B10 B 7.94 pIC50 11.6 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20764-20769 [PMID:18087047]
Aldo-keto reductase family 1 member C21 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075270] [UniProtKB: Q91WR5]
ChEMBL Inhibition of mouse recombinant AKR1C21 B 4.66 pKi 22000 nM Ki Bioorg. Med. Chem. (2008) 16: 3245-3254 [PMID:18165015]
ChEMBL Inhibition of mouse recombinant AKR1C21 B 4.32 pIC50 48000 nM IC50 Bioorg. Med. Chem. (2008) 16: 3245-3254 [PMID:18165015]
aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
ChEMBL In vitro inhibitory activity against recombinant human aldose reductase (ALR2) was determined B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2003) 46: 5208-5221 [PMID:14613323]
ChEMBL Inhibitory Activity against Human recombinant Aldose Reductase (wild type) B 7.33 pIC50 47 nM IC50 J. Med. Chem. (2000) 43: 1062-1070 [PMID:10737739]
GtoPdb - - 7.33 pIC50 47 nM IC50 J Med Chem (2000) 43: 1062-70 [PMID:10737739]
ChEMBL Inhibition of human recombinant aldose reductase B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. (2008) 16: 3245-3254 [PMID:18165015]
ChEMBL Inhibitory activity against aldose reductase enzyme B 7.46 pIC50 35 nM IC50 J. Med. Chem. (2003) 46: 417-426 [PMID:12540241]
ChEMBL Compound was evaluated In vitro for inhibition of aldose reductase activity by 50% in dog RBC B 7.62 pIC50 23.9 nM IC50 J. Med. Chem. (1994) 37: 2043-2058 [PMID:8027986]
ChEMBL In vitro inhibition of recombinant human aldose reductase expressed in Escherichia coli B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2005) 48: 3141-3152 [PMID:15857120]
ChEMBL Inhibition of N-terminal 6His-tagged human aldose reductase expressed in Escherichia coli BL21(DE3) mediated NADPH linked pyridine-3-aldehyde reduction B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. (2010) 18: 2485-2490 [PMID:20304656]
ChEMBL Inhibition of human AKR1B1 assessed as decrease in glyceraldehyde reduction B 8 pIC50 10 nM IC50 J Med Chem (2017) 60: 8441-8455 [PMID:28976752]
Aldose reductase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4559] [UniProtKB: P80276]
ChEMBL Inhibition of pig kidney aldose reductase (ALR2) B 4.8 pIC50 16000 nM IC50 J. Med. Chem. (2003) 46: 5619-5627 [PMID:14667216]
ChEMBL Inhibition of aldose reductase from pig lenses B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2004) 47: 5076-5084 [PMID:15456251]
ChEMBL Inhibitory concentration against porcine lens aldose reductase (AR) with DL-glyceraldehyde as the substrate B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1677-1682
ChEMBL In vitro inhibitory activity against aldose reductase in porcine lens. B 7.82 pIC50 15 nM IC50 J. Med. Chem. (1998) 41: 4118-4129 [PMID:9767647]
Aldose reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3081] [UniProtKB: P16116]
ChEMBL Evaluated for inhibition of Aldose reductase 2 B 7.02 pIC50 96 nM IC50 J. Med. Chem. (1996) 39: 4396-4405 [PMID:8893834]
ChEMBL In vitro inhibition of aldose reductase from the partially purified bovine lens B 7.46 pIC50 35 nM IC50 J. Med. Chem. (1990) 33: 2892-2899 [PMID:2120443]
ChEMBL Inhibition of bovine lens aldose reductase with DL-glyceraldehyde as substrate B 7.46 pIC50 35 nM IC50 J. Med. Chem. (1984) 27: 255-256 [PMID:6422042]
ChEMBL In vitro inhibition of bovine lens aldose reductase B 7.46 pIC50 35 nM IC50 J. Med. Chem. (1989) 32: 757-765 [PMID:2539477]
ChEMBL inhibition of aldose reductase activity was measured on partially purified bovine lens preparations incubated in presence of 50 mM glucose. B 7.47 pIC50 34 nM IC50 J. Med. Chem. (1991) 34: 2504-2520 [PMID:1908522]
ChEMBL In vitro inhibition of aldose reductase in partially purified bovine lens preparation at a concentration of 10e -8M. B 7.48 pIC50 33 nM IC50 J. Med. Chem. (1991) 34: 1492-1503 [PMID:1901912]
ChEMBL In vitro inhibition of aldose reductase activity in a partially purified bovine lens preparation B 7.48 pIC50 33 nM IC50 J. Med. Chem. (1994) 37: 2043-2058 [PMID:8027986]
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
ChEMBL Inhibition of rat AKR1B4 B 6 pIC50 1000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20764-20769 [PMID:18087047]
ChEMBL In vitro inhibitory activity against L-Hexonate Dehydrogenase (L-HDH) from rat kidney (RK) B 6.02 pIC50 950 nM IC50 J. Med. Chem. (1991) 34: 3229-3234 [PMID:1956041]
ChEMBL Inhibition of aldose reductase (or polyol accumulation) in isolated rat sciatic nerve by compound at 10e-5 M concentration B 6.27 pIC50 540 nM IC50 J. Med. Chem. (1989) 32: 757-765 [PMID:2539477]
ChEMBL Inhibition of Albino rat eye lens ALR2 assessed as NADPH oxidation by spectrophotometry B 7.3 pIC50 50 nM IC50 Eur. J. Med. Chem. (2010) 45: 909-914 [PMID:19962793]
ChEMBL Inhibition of Sprague-Dawley rat lens ALR2 using D,L-glyceraldehyde as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by spectrophotometric method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2017) 25: 3068-3076 [PMID:28392277]
ChEMBL In vitro inhibitory activity against aldose reductase (ALR2) from rat lens extraction. B 7.3 pIC50 50 nM IC50 J. Med. Chem. (2003) 46: 1419-1428 [PMID:12672241]
ChEMBL Inhibitory concentration to aldose reductase (ALR-2) obtained from rat lens B 7.3 pIC50 50 nM IC50 J. Med. Chem. (2001) 44: 4359-4369 [PMID:11728182]
ChEMBL In vitro inhibitory activity against aldose reductase (ALR2) from rat lens extraction. B 7.34 pIC50 46 nM IC50 J. Med. Chem. (2003) 46: 1419-1428 [PMID:12672241]
ChEMBL Inhibitory activity measured against rat lens aldose reductase using 3-pyridinecarboxaldehyde as substrate B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (1991) 34: 1011-1018 [PMID:1900532]
ChEMBL In vitro inhibition of Aldose reductase (AR) from rat lens (RL) B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1991) 34: 3229-3234 [PMID:1956041]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]