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ChEMBL ligand: CHEMBL10372 (Alond, CP-73,850, CP-73850, Zopolrestat) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Aldehyde reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2246] [UniProtKB: P14550] | ||||||||
ChEMBL | In vitro inhibition of recombinant human aldehyde reductase | B | 4.41 | pIC50 | 38600 | 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 | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem (2010) 18: 2485-2490 [PMID:20304656] |
Aldo-keto reductase family 1 member B10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5983] [UniProtKB: O60218] | ||||||||
ChEMBL | Inhibition of recombinant AKR1B10 assessed as NADP+ dependent reduction of DL-glyceraldehyde by fluorescence assay | B | 5.63 | pIC50 | 2360 | nM | IC50 | J Med Chem (2012) 55: 2311-2323 [PMID:22263837] |
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 | 6.21 | pIC50 | 620 | nM | IC50 | Bioorg Med Chem (2010) 18: 2485-2490 [PMID:20304656] |
aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121] | ||||||||
ChEMBL | Compound was tested for the rate of reduction of glyceraldehyde by human placental aldose reductase. | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
GtoPdb | In vitro inhibition of recombinant human aldehyde reductase | - | 4.41 | pIC50 | 38600 | nM | IC50 | J Med Chem (2005) 48: 3141-52 [PMID:15857120] |
ChEMBL | Compound was tested for the inhibition of the human placental aldose reductase using the substrate as glyceraldehyde. | B | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
ChEMBL | Inhibition of N-terminal 6His-tagged human aldose reductase expressed in Escherichia coli BL21(DE3) mediated NADPH linked pyridine-3-aldehyde reduction | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2010) 18: 2485-2490 [PMID:20304656] |
ChEMBL | Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 1M DMSO followed by compound addition by DMSO-perturbation assay | B | 7.28 | pIC50 | 52.9 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126815-126815 [PMID:31744675] |
ChEMBL | Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.7M DMSO followed by compound addition by DMSO-perturbation assay | B | 7.37 | pIC50 | 42.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126815-126815 [PMID:31744675] |
ChEMBL | Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.3M DMSO followed by compound addition by DMSO-perturbation assay | B | 7.42 | pIC50 | 37.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126815-126815 [PMID:31744675] |
ChEMBL | Inhibitory Activity against Human recombinant Aldose Reductase (wild type) | B | 7.44 | pIC50 | 36.4 | nM | IC50 | J Med Chem (2000) 43: 1062-1070 [PMID:10737739] |
ChEMBL | Inhibition of human recombinant aldose reductase | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2008) 16: 3245-3254 [PMID:18165015] |
ChEMBL | Inhibition of recombinant AKR1B1 assessed as NADP+ dependent reduction of DL-glyceraldehyde by fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2012) 55: 2311-2323 [PMID:22263837] |
ChEMBL | Inhibition of recombinant human AKR1B1 using D,L-glyceraldehyde as substrate | B | 7.61 | pIC50 | 24.8 | nM | IC50 | Bioorg Med Chem (2017) 25: 6353-6360 [PMID:29074349] |
ChEMBL | In vitro inhibition of recombinant human aldose reductase expressed in Escherichia coli | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2005) 48: 3141-3152 [PMID:15857120] |
ChEMBL | Inhibitory activity against aldose reductase isolated from human placenta | B | 8.32 | pIC50 | 4.8 | nM | IC50 | J Med Chem (1992) 35: 2155-2162 [PMID:1613743] |
ChEMBL | In vitro inhibitroy concentration against Aldose reductase incubated at 24 degree C for 15 minutes in pH 7.0 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2005) 48: 6326-6339 [PMID:16190759] |
ChEMBL | Inhibition of human recombinant Aldose reductase in streptozotocin diabetic rat | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2003) 46: 2283-2286 [PMID:12773033] |
ChEMBL | Inhibition of human placental aldose reductase using glyceraldehyde as substrate in presence of NADPH | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2017) 138: 1002-1033 [PMID:28759875] |
ChEMBL | Inhibition of aldose reductase (aldo-keto reductase, AKR1B1) isolated from human placenta. | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
ChEMBL | Inhibitory activity against aldose reductase enzyme | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2003) 46: 417-426 [PMID:12540241] |
ChEMBL | In vitro inhibitory activity against aldose reductase isolated from human placenta | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1992) 35: 457-465 [PMID:1738141] |
ChEMBL | Inhibition of human placenta Aldose reductase | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008] |
ChEMBL | Compound was tested for the inhibition of the human placental aldose reductase using the substrate as glyceraldehyde. | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943] | ||||||||
ChEMBL | Compound was tested for the inhibition of the rat lens aldose reductase using the substrate as glyceraldehyde | B | 7.39 | pIC50 | 41 | nM | IC50 | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
ChEMBL | Compound was tested for the inhibition of the rat lens aldose reductase using the substrate as glucose. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1991) 34: 108-122 [PMID:1899452] |
ChEMBL | Inhibition of Wistar rat lens aldose reductase 2 | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2008) 16: 4908-4920 [PMID:18395454] |
ChEMBL | Inhibition of Wistar rat lens aldose reductase using D,L-glyceraldehyde as substrate incubated for 1 min measured for 4 mins by spectrophotometry | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2015) 58: 2649-2657 [PMID:25695864] |
Aldose reductase-related protein 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421523] [UniProtKB: Q5RJP0] | ||||||||
ChEMBL | Inhibition of Wistar rat kidney aldehyde reductase using D-glucuronate as substrate by spectrophotometry | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (2015) 58: 2649-2657 [PMID:25695864] |
Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760] | ||||||||
ChEMBL | Inhibition of human Glyoxalase-1 using GSH and MGO as substrate by Dixon plot analysis | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2020) 28: 115243-115243 [PMID:31879183] |
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]