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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 33:
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]