allopurinol [Ligand Id: 6795] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1467 (Allopurinol, Allopurinolum, Aloral, Aluline 100, Aluline 300, BW 56-158, BW-56-158, Caplenal, Cosuric, Hamarin 100, Hamarin 300, Ledopur, Lopurin, NSC-101655, NSC-1390, Suspendol, Takanarumin, Uricto, Xanthomax-100, Xanthomax-300, Zyloprim, Zyloric, Zyloric-300) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay | B | 4.11 | pKd | 77000 | nM | Kd | ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869] |
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | null: A commercially available P450-GLO Assay kit (Promega Corporation, Madison Wis.) is used to screen various compounds for CYP3A4A inhibition activity. CYP3A4A is thought to be one of the primary CYP isoforms responsible for retinoic acid metabolism in the skin. Three benchmark agents, liarozole, climbazole, and ketoconazole, were assessed for CYP3A4 inhibition to confirm that the inhibition activity (the IC50 for CYP3A4 inhibition) measured by the assay corresponds to the activity reported by the published literature. The results show that the substituted azole compounds having the specific structure set forth herein are CYP inhibitors, and thus function as RAMBAs. | B | 5 | pIC50 | >10000 | nM | IC50 | US-9138393-B2. Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin (2015) |
| ChEMBL | In vitro CYP3A4 Inhibition Assay: Cytochrome P450 is a large and diverse group of enzymes that catalyze the oxidation of organic substances. Some members of the CYP family contribute to the elimination of ATRA by catalyzing its 4-hydroxylation in the mammalian liver and skin, including that of humans as well as swine. Applicant evaluated the potential RAMBA activity of several azoles using pig liver microsomes, a rich source of CYP activity, comprising many different CYP 450 isoforms. Therefore, this approach, while a reasonable way to assess CYP inhibitors with broad activities may or may not be the best way to discover RAMBAs with selectivity for the skin, which has a much more narrow complement of CYP expression. As understanding in this area has progressed, a more specific CYP inhibition assay can be used to provide better predictivity of activity in human skin. Nevertheless, this assay may still be used as a general predictor of overall CYP activity. | B | 5 | pIC50 | >10000 | nM | IC50 | US-9144538-B2. Cosmetic compositions containing substituted azole and methods for alleviating the signs of photoaged skin (2015) |
| Shiga toxin subunit A in Shigella dysenteriae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879822] [UniProtKB: Q9FBI2] | ||||||||
| ChEMBL | Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay | B | 4.62 | pIC50 | 23900 | nM | IC50 | J Med Chem (2016) 59: 10763-10773 [PMID:27933947] |
| xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989] | ||||||||
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) | B | 5.14 | pKi | 7300 | nM | Ki | Eur J Med Chem (2014) 84: 206-239 [PMID:25019478] |
| GtoPdb | - | - | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (1996) 39: 2529-35 [PMID:8691450] |
| ChEMBL | Inhibitory activity against Xanthine Oxidase | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (1996) 39: 2529-2535 [PMID:8691450] |
| ChEMBL | Non-competitive inhibition of xanthine oxidase (unknown origin) by Lineweaver-Burk plot analysis | B | 5.81 | pKi | 1550 | nM | Ki | Bioorg Med Chem (2016) 24: 226-231 [PMID:26712096] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) | B | 6.15 | pKi | 700 | nM | Ki | Eur J Med Chem (2019) 166: 186-196 [PMID:30769179] |
| ChEMBL | Competitive inhibition of xanthine oxidase (unknown origin) assessed as inhibitory constant of enzyme-substrate complex using xanthine as substrate at varying concentrations preincubated for 15 mins followed by substrate addition by UV spectrophotometric analysis | B | 6.15 | pKi | 700 | nM | Ki | Eur J Med Chem (2022) 229: 114086-114086 [PMID:34992040] |
| ChEMBL | Inhibition of human xanthine oxidase | B | 7 | pKi | 100 | nM | Ki | J Nat Prod (2014) 77: 1693-1699 [PMID:25060641] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method | B | 4.3 | pIC50 | 50150 | nM | IC50 | Bioorg Med Chem (2017) 25: 3562-3566 [PMID:28511908] |
| ChEMBL | Inhibition of xanthine oxidase | B | 4.46 | pIC50 | 34910 | nM | IC50 | J Nat Prod (2005) 68: 1615-1621 [PMID:16309309] |
| ChEMBL | Inhibition of Xanthine oxidase | B | 4.46 | pIC50 | 34910 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2777-2780 [PMID:12873513] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 30 mins by UV-Vis spectrophotometric assay | B | 4.5 | pIC50 | 31620 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) | B | 4.5 | pIC50 | 31620 | nM | IC50 | Eur J Med Chem (2018) 156: 394-429 [PMID:30015075] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 4 mins by UV-Vis spectrophotometric assay | B | 4.51 | pIC50 | 30700 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of xanthine oxidase | B | 4.61 | pIC50 | 24400 | nM | IC50 | Eur J Med Chem (2008) 43: 771-780 [PMID:17692432] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) by SAR analysis | B | 4.61 | pIC50 | 24300 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of xanthine oxidase by spectrophotometry | B | 4.62 | pIC50 | 24200 | nM | IC50 | J Nat Prod (1999) 62: 1053-1055 [PMID:10425142] |
| ChEMBL | Inhibition of xanthine oxidase assessed as formation of formazan at 16 ug/ml after 2 hrs by spectrophotometry | B | 4.63 | pIC50 | 23500 | nM | IC50 | Bioorg Med Chem (2009) 17: 3414-3425 [PMID:19362850] |
| ChEMBL | Inhibition of xanthine oxidase assessed as decrease of superoxide generation | B | 4.66 | pIC50 | 21800 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5006-5009 [PMID:18722771] |
| ChEMBL | Inhibition of xanthine oxidase assessed as decrease of uric acid generation | B | 4.94 | pIC50 | 11400 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5006-5009 [PMID:18722771] |
| ChEMBL | Inhibition of xanthine oxidase assessed as uric acid formation by spectrophotometry | B | 4.99 | pIC50 | 10340 | nM | IC50 | Eur J Med Chem (2008) 43: 862-871 [PMID:17706325] |
| ChEMBL | Inhibition of xanthine oxidase | B | 5.01 | pIC50 | 9820 | nM | IC50 | J Nat Prod (2006) 69: 1089-1091 [PMID:16872152] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate incubated for 15 mins followed by substrate addition by spectrophotometric analysis | B | 5.08 | pIC50 | 8370 | nM | IC50 | Eur J Med Chem (2022) 227: 113928-113928 [PMID:34688012] |
| ChEMBL | Inhibition of human xanthine oxidase | B | 5.11 | pIC50 | 7820 | nM | IC50 | Bioorg Med Chem (2007) 15: 3450-3456 [PMID:17379526] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition by UV spectrophotometric analysis | B | 5.12 | pIC50 | 7590 | nM | IC50 | Eur J Med Chem (2022) 229: 114086-114086 [PMID:34992040] |
| ChEMBL | Inhibition of xanthine oxidase | B | 5.13 | pIC50 | 7450 | nM | IC50 | J Nat Prod (2005) 68: 189-193 [PMID:15730241] |
| ChEMBL | Inhibitory activity against Xanthine Oxidase | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (1996) 39: 2529-2535 [PMID:8691450] |
| ChEMBL | Inhibition of xanthine oxidase using xanthine as substrate at 30 mins by spectrophotometric analysis | B | 5.38 | pIC50 | 4190 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7543-7546 [PMID:23122864] |
| GtoPdb | - | - | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (1996) 39: 2529-35 [PMID:8691450] |
| ChEMBL | Inhibition of Xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 3 mins followed by substrate addition measured every 15 secs for 7 mins by spectrophotometry | B | 5.44 | pIC50 | 3610 | nM | IC50 | Eur J Med Chem (2016) 124: 637-648 [PMID:27614410] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) at 30 uM using xanthine as substrate preincubated for 5 mins followed by substrate addition measured every min for 10 mins by spectrophotometric method relative to control | B | 5.5 | pIC50 | 3170 | nM | IC50 | Eur J Med Chem (2018) 143: 829-842 [PMID:29223098] |
| ChEMBL | Inhibition of xanthine oxidase | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Nat Prod (2010) 73: 992-994 [PMID:20384317] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by spectrophotometric analysis | B | 5.54 | pIC50 | 2900 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2778-2781 [PMID:26022844] |
| ChEMBL | Inhibition of Xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 1 to 5 mins followed by substrate addition | B | 5.54 | pIC50 | 2900 | nM | IC50 | Bioorg Med Chem (2018) 26: 1653-1664 [PMID:29472126] |
| ChEMBL | Inhibition of Xanthine oxidase | B | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2558-2560 [PMID:17346963] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) | B | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126944-126944 [PMID:31924495] |
| ChEMBL | Inhibtion Assay : Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P: Int J Biochem. 10:317-9, 1979) with minor variations. The procedure was internally standardized using allopurinol and DPI as controls for all experiments after determination of their optimal inhibitory concentrations. Experiments on test compounds were performed in triplicate in multi-well plates using 10 concentrations of each compound that ranged over a 3-fold dilution. | B | 5.67 | pIC50 | 2130 | nM | IC50 | US-9428466-B2. Methods for reducing uric acid levels using barbiturate derivatives (2016) |
| ChEMBL | Inhibition of xanthine oxidase | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Nat Prod (2008) 71: 1027-1031 [PMID:18512985] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate measured at every 1 mins up to 5 mins | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of xanthine oxidase | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem (2008) 16: 7270-7276 [PMID:18606546] |
| ChEMBL | Inhibition of xanthine oxidase activity assessed as uric acid formation pretreated for 15 mins before substrate addition measured after 5 mins | B | 5.72 | pIC50 | 1900 | nM | IC50 | Eur J Med Chem (2011) 46: 1222-1231 [PMID:21345544] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate pretreated for 10 mins followed by substrate addition measured every 2 mins for 6 mins | B | 6 | pIC50 | 1000 | nM | IC50 | J Nat Prod (2017) 80: 2778-2786 [PMID:28972762] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate assessed as inhibition of uric acid formation after 30 mins by spectrophotometric method | B | 6.02 | pIC50 | 950 | nM | IC50 | Eur J Med Chem (2016) 119: 197-217 [PMID:27162124] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) at 10 uM using xanthine as substrate | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2022) 54: 116560-116560 [PMID:34923389] |
| ChEMBL | Inhibition of xanthine oxidase assessed as decrease in uric acid production by spectrophotometry | B | 6.62 | pIC50 | 240 | nM | IC50 | J Nat Prod (1998) 61: 71-76 [PMID:9461655] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2016) 24: 578-587 [PMID:26762836] |
| ChEMBL | Inhibition of XOD | B | 6.74 | pIC50 | 180 | nM | IC50 | J Nat Prod (2009) 72: 1198-1201 [PMID:19476336] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 10 mins | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation preincubated for 5 mins followed by addition of xanthine substrate measured every minute up to 8 mins | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem (2017) 25: 166-174 [PMID:28340987] |
| Xanthine dehydrogenase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3649] [UniProtKB: P80457] | ||||||||
| ChEMBL | Binding affinity to bovine milk xanthine oxidase assessed as reduction in conversion of 4-HPP to 4,6-diHPP by measuring cytochrome c reduction by spectrophotometric assay | B | 9.27 | pKd | 0.54 | nM | Kd | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Mixed-type inhibition of bovine milk xanthine oxidase using hypoxanthine as substrate by Lineweaver-Burk plot analysis | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1976) 19: 291-296 [PMID:2778] |
| ChEMBL | Mixed-type inhibition of bovine milk xanthine oxidase using xanthine as substrate by Lineweaver-Burk plot analysis | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (1976) 19: 291-296 [PMID:2778] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method | B | 4.36 | pIC50 | 44000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2874-2879 [PMID:27133595] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase pre-incubated for 30 mins followed by xanthine addition and measured every 30 secs for 5 mins by spectrophotometry | B | 4.71 | pIC50 | 19600 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3602-3606 [PMID:28655421] |
| ChEMBL | Inhibition of bovine XOD assessed as inhibition of uric acid formation using xanthine as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured for 30 mins by microplate reader analysis | B | 4.9 | pIC50 | 12520 | nM | IC50 | Eur J Med Chem (2022) 237: 114379-114379 [PMID:35468514] |
| ChEMBL | Inhibition of bovine xanthine oxidase using xanthine as substrate measured for 6 mins at 25 degC by spectrophotometry | B | 4.95 | pIC50 | 11230 | nM | IC50 | Eur J Med Chem (2014) 75: 289-296 [PMID:24556143] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate assessed as decrease in uric acid formation preincubated for 5 mins | B | 4.95 | pIC50 | 11100 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 495-500 [PMID:24388807] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate pretreated for 5 mins followed by substrate addition measured by UV-vis spectrophotometric method | B | 4.95 | pIC50 | 11100 | nM | IC50 | Eur J Med Chem (2017) 131: 14-28 [PMID:28286211] |
| ChEMBL | Inhibition of bovine xanthine oxidase using xanthine as substrate preincubated for 3 mins followed by substrate addition and measured for every 15 secs for 7 mins by spectrophotometric analysis | B | 4.97 | pIC50 | 10610 | nM | IC50 | Eur J Med Chem (2018) 151: 849-860 [PMID:29684895] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid levels using xanthine as substrate after 120 mins by spectrophotometry | B | 5.01 | pIC50 | 9800 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 729-732 [PMID:28131711] |
| ChEMBL | Inhibition of bovine XO assessed as inhibition of uric acid formation using xanthine as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured for 2 mins by spectrophotometry | B | 5.01 | pIC50 | 9800 | nM | IC50 | Bioorg Med Chem Lett (2022) 60: 128582-128582 [PMID:35077850] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 5 mins followed by substrate addition by UV-visible spectrophotometry | B | 5.06 | pIC50 | 8690 | nM | IC50 | Medchemcomm (2019) 10: 128-147 [PMID:30931089] |
| ChEMBL | Inhibition of bovine milk XO assessed as decrease in uric acid formation after 5 mins by UV-spectrophotometric analysis | B | 5.07 | pIC50 | 8500 | nM | IC50 | Bioorg Med Chem (2012) 20: 5649-5657 [PMID:22901670] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 10 mins followed by substrate addition by UV spectrophotometric method | B | 5.07 | pIC50 | 8500 | nM | IC50 | Eur J Med Chem (2017) 141: 362-372 [PMID:29032030] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 5 mins followed by substrate addition by UV-Vis spectrophotometric assay | B | 5.08 | pIC50 | 8310 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of bovine Xanthine oxidase assessed as decrease in uric acid production preincubated at 293 nM of compound for 5 mins by spectrophotometry | B | 5.08 | pIC50 | 8300 | nM | IC50 | Bioorg Med Chem (2011) 19: 1950-1958 [PMID:21353569] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as decrease of uric acid formation preincubated for 5 mins by UV-visible spectrophotometric analysis | B | 5.08 | pIC50 | 8300 | nM | IC50 | Bioorg Med Chem (2011) 19: 5569-5576 [PMID:21862335] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured every 30 secs for 2 mins by spectrophotometric method | B | 5.12 | pIC50 | 7590.2 | nM | IC50 | Eur J Med Chem (2019) 181: 111558-111558 [PMID:31369933] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 25 mins followed by substrate addition measured at first 2 mins by spectrophotometric analysis | B | 5.12 | pIC50 | 7590 | nM | IC50 | Eur J Med Chem (2020) 190: 112077-112077 [PMID:32014678] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate incubated for 15 mins followed by substrate addition and measured at 30 sec interval for 2 mins by spectrophotometrically | B | 5.12 | pIC50 | 7590 | nM | IC50 | Eur J Med Chem (2019) 181: 111559-111559 [PMID:31376568] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid production using xanthine as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis | B | 5.12 | pIC50 | 7560 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3812-3816 [PMID:28693909] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation preincubated for 5 mins followed by xanthine addition and measured after 20 mins by spectrophotometry | B | 5.19 | pIC50 | 6430 | nM | IC50 | Bioorg Med Chem (2019) 27: 1818-1823 [PMID:30885567] |
| ChEMBL | Inhibition of bovine xanthine oxidase assessed as uric acid formation using xanthine as substrate after 30 mins by spectrophotometric analysis | B | 5.24 | pIC50 | 5700 | nM | IC50 | Bioorg Med Chem (2012) 20: 2930-2939 [PMID:22483591] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 15 mins followed by substrate addition measured for every 30 sec by spectrophotometric analysis | B | 5.26 | pIC50 | 5462 | nM | IC50 | Bioorg Med Chem (2021) 38: 116117-116117 [PMID:33838610] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1976) 19: 291-296 [PMID:2778] |
| ChEMBL | Inhibition of bovine xanthine oxidase-mediated uric acid production after 30 mins by spectrophotometric analysis | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 834-838 [PMID:23265878] |
| ChEMBL | Inhibition of cow milk xanthine oxidoreductase using hypoxanthine by spectrophotometry | B | 5.38 | pIC50 | 4200 | nM | IC50 | Eur J Med Chem (2017) 140: 20-30 [PMID:28918097] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 3 hrs followed by substrate addition measured after 1 min by UV spectrophotometric assay | B | 5.45 | pIC50 | 3530 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of bovine xanthine oxidase | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1977) 20: 1189-1193 [PMID:926119] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 3 hrs followed by substrate addition by UV-Vis spectrophotometric assay | B | 5.53 | pIC50 | 2930 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate pretreated for 15 mins followed by substrate addition measured after 8 mins | B | 5.59 | pIC50 | 2600 | nM | IC50 | Bioorg Med Chem (2018) 26: 536-542 [PMID:29274704] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate measured for 20 mins by microplate assay | B | 5.6 | pIC50 | 2520 | nM | IC50 | RSC Med Chem (2020) 11: 518-527 [PMID:33479653] |
| ChEMBL | Inhibition of bovine milk XOR-mediated uric acid formation after 15 mins by spectrophotometer | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6225-6229 [PMID:19783139] |
| ChEMBL | Inhibition of bovine xanthine oxidase using xanthine as substrate preincubated for 10 mins followed by substrate addition measured for 15 mins by spectrophotometric method | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem (2017) 25: 2351-2371 [PMID:28302506] |
| ChEMBL | Inhibition of cow milk xanthine oxidase | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Nat Prod (1989) 52: 210-211 [PMID:2723668] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid production using xanthine as substrate after 10 mins by HPLC analysis | B | 6 | pIC50 | 1000 | nM | IC50 | J Nat Prod (2019) 82: 205-210 [PMID:30719922] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase by spectrophotometry | B | 6.14 | pIC50 | 730 | nM | IC50 | Bioorg Med Chem (2011) 19: 211-220 [PMID:21163661] |
| ChEMBL | In vitro inhibitory concentration against Xanthine oxidase | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 879-882 [PMID:11294382] |
| ChEMBL | Inhibition of bovine milk xanthine-oxygen reductase using xanthine as substrate by spectrophotometric assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2017) 135: 491-516 [PMID:28478180] |
| ChEMBL | Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by UV-VIS spectrophotometric analysis | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2018) 143: 577-582 [PMID:29207340] |
| xanthine dehydrogenase in Human [GtoPdb: 2646] [UniProtKB: P47989] | ||||||||
| GtoPdb | - | - | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (1996) 39: 2529-35 [PMID:8691450] |
| GtoPdb | - | - | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (1996) 39: 2529-35 [PMID:8691450] |
| xanthine dehydrogenase/Xanthine dehydrogenase/oxidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075246] [GtoPdb: 2646] [UniProtKB: P22985] | ||||||||
| ChEMBL | Inhibition of rat liver xanthine oxidase after 2 hrs by spectrophotometry | B | 4.67 | pIC50 | 21200 | nM | IC50 | J Med Chem (2009) 52: 7732-7752 [PMID:19673490] |
| ChEMBL | Inhibition of Wistar albino rat xanthine oxidase isolated from liver using xanthine as substrate incubated for 15 mins prior to substrate addition by spectrophotometric analysis | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem (2013) 21: 365-372 [PMID:23177727] |
| ChEMBL | Inhibition of rat liver xanthine oxidase by spectrophotometry | B | 6.12 | pIC50 | 753 | nM | IC50 | Bioorg Med Chem (2011) 19: 211-220 [PMID:21163661] |
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]
