zonisamide [Ligand Id: 7047] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL750 (AD-810, CI-912, Excegran, N03AX15, PD-110843, Zonegran, Zonisade, Zonisamida, Zonisamide, Zonisamide mylan) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| AGAP002992-PA in Anopheles gambiae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399914] [UniProtKB: Q5TU56] | ||||||||
| ChEMBL | Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 6.58 | pKi | 263 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| Alpha carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02] | ||||||||
| ChEMBL | Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
| ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| Amine oxidase [flavin-containing] in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1681610] [UniProtKB: Q6NSN2] | ||||||||
| ChEMBL | Competitive inhibition of zebrafish MAO by spectrophotometry | B | 4.51 | pKi | 30800 | nM | Ki | J Med Chem (2011) 54: 909-912 [PMID:21175212] |
| Monoamine oxidase B/Amine oxidase [flavin-containing] B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of MAO-B (unknown origin) | B | 4.51 | pKi | 30800 | nM | Ki | Eur J Med Chem (2018) 145: 445-497 [PMID:29335210] |
| ChEMBL | Competitive inhibition of human MAO B by spectrophotometry | B | 5.51 | pKi | 3100 | nM | Ki | J Med Chem (2011) 54: 909-912 [PMID:21175212] |
| ChEMBL | Competitive inhibition of human MAO-B | B | 5.51 | pKi | 3100 | nM | Ki | Eur J Med Chem (2018) 145: 445-497 [PMID:29335210] |
| Monoamine oxidase B/Amine oxidase [flavin-containing] B in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3050] [GtoPdb: 2490] [UniProtKB: Q8BW75] | ||||||||
| ChEMBL | Inhibition of MAO-B in mouse brain assessed as reduction in H2O2 production incubated for 30 mins using benzylamine as substrate by Amplex red reagent based fluorescence assay | B | 4.61 | pIC50 | 24800 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126677-126677 [PMID:31537422] |
| Monoamine oxidase B/Amine oxidase [flavin-containing] B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | Competitive inhibition of rat MAO B by spectrophotometry | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (2011) 54: 909-912 [PMID:21175212] |
| ChEMBL | Competitive inhibition of rat MAO-B | B | 5.54 | pKi | 2900 | nM | Ki | Eur J Med Chem (2018) 145: 445-497 [PMID:29335210] |
| Astrosclerin-3 in Astrosclera willeyana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944499] [UniProtKB: A6YCJ1] | ||||||||
| ChEMBL | Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 6.78 | pKi | 165 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| Beta-carbonic anhydrase 1 in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7] | ||||||||
| ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay | B | 4.54 | pKi | 28680 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3] | ||||||||
| ChEMBL | Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| Carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24] | ||||||||
| ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 6.19 | pKi | 645 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| Carbonic anhydrase in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4211] [UniProtKB: O24855] | ||||||||
| ChEMBL | Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay | B | 6.64 | pKi | 231 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| ChEMBL | Inhibition of Helicobacter pylori recombinant CA | B | 6.66 | pKi | 218 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71] | ||||||||
| ChEMBL | Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay | B | 6.03 | pKi | 942 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 6.03 | pKi | 942 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
| ChEMBL | Inhibition of Candida albicans recombinant Nce103 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 6.03 | pKi | 940 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| Carbonic anhydrase in Candida glabrata CBS 138 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6] | ||||||||
| ChEMBL | Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 6.94 | pKi | 114 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2647-2652 [PMID:23511020] |
| Carbonic anhydrase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5931] [UniProtKB: P53615] | ||||||||
| ChEMBL | Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay | B | 6.97 | pKi | 106 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| carbonic anhydrase 1/Carbonic anhydrase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 1 esterase activity using 4-nitrophenylacetate as substrate | B | 4.83 | pKi | 14800 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1352-1357 [PMID:22230050] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | B | 4.83 | pKi | 14800 | nM | Ki | Eur J Med Chem (2012) 49: 68-73 [PMID:22245047] |
| ChEMBL | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| GtoPdb | - | - | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| ChEMBL | Inhibition of human cloned CA1 by CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human cloned CA1 by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| ChEMBL | Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.5 | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841] |
| ChEMBL | Inhibition of human recombinant CA1 cytosolic isoform by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 after 15 mins by CO2 hydrase assay at pH 7.5 | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2011) 19: 1847-1851 [PMID:21377369] |
| ChEMBL | Inhibition of human recombinant alpha-carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3170-3173 [PMID:19435663] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 preincubated with compound for 15 mins by carbon dioxide hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant full length CA1 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2011) 19: 7003-7007 [PMID:22041171] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| ChEMBL | Inhibition of human recombinant full length CA1-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| ChEMBL | Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
| ChEMBL | Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| ChEMBL | Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| ChEMBL | Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
| ChEMBL | Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
| ChEMBL | Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
| ChEMBL | Inhibition of human recombinant CA1 | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2006) 49: 5544-5551 [PMID:16942027] |
| ChEMBL | Known Inhibitors of Carbonic Anhydrase: Compounds which are CAIs are well known in the art, see for example, Pastorekova et al, Journal of Enzyme Inhibition and Medicinal Chemistry, 19(3), 199-229, 2004. Methods for determining the carbonic anhydrase inhibitory activity of a compound, i.e. whether a compound can be classified as a CAI, are known in the art and may usefully identify further compounds which may be suitable for use in the present invention. Exemplary methods and levels of activity required for consideration as CAIs are described in US 20020022245 and the references cited therein, the contents of which are incorporated herein by reference, in particular Supuran et al, European Journal of Medicinal Chemistry, 1998, 33, 577-594 and Scozzafava et al, Journal of Medicinal Chemistry, 1999, 42 25, 3690-3700). | B | 7.46 | pIC50 | 35 | nM | IC50 | US-10172837-B2. Insulin sensitisers and methods of treatment (2019) |
| carbonic anhydrase 12/Carbonic anhydrase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibitory constant against catalytic domain of human carbonic anhydrase XII | B | 4.96 | pKi | 11000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| ChEMBL | Inhibition of human cloned CA12 catalytic domain by stopped flow CO2 hydration assay | B | 4.96 | pKi | 11000 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA12 by stopped flow CO2 hydrase assay | B | 4.96 | pKi | 11000 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 4.96 | pKi | 11000 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay | B | 4.96 | pKi | 11000 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| GtoPdb | - | - | 4.96 | pKi | 11000 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
| ChEMBL | Inhibition of recombinant human CA12 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| carbonic anhydrase 13/Carbonic anhydrase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1] | ||||||||
| ChEMBL | Inhibition of human recombinant CA13 by stopped flow CO2 hydrase assay | B | 6.37 | pKi | 430 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 14/Carbonic anhydrase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7] | ||||||||
| ChEMBL | Inhibitory constant against human carbonic anhydrase XIV in CO2 hydrase assay | B | 5.28 | pKi | 5250 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| ChEMBL | Inhibition of human recombinant CA14 by stopped flow CO2 hydrase assay | B | 5.28 | pKi | 5250 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human carbonic anhydrase 14 preincubated with compound for 15 mins by carbon dioxide hydration assay | B | 5.28 | pKi | 5250 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant full length carbonic anhydrase 14 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.28 | pKi | 5250 | nM | Ki | Bioorg Med Chem (2011) 19: 7003-7007 [PMID:22041171] |
| ChEMBL | Inhibition of human recombinant full length CA14-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 5.28 | pKi | 5250 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23] | ||||||||
| ChEMBL | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay | B | 6.2 | pKi | 634 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of mouse recombinant CA15 by stopped flow CO2 hydrase assay | B | 6.2 | pKi | 634 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| Carbonic anhydrase 2 in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9] | ||||||||
| ChEMBL | Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | B | 6.06 | pKi | 876 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
| carbonic anhydrase 2/Carbonic anhydrase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 2 | B | 7.32 | pKd | 47.6 | nM | Kd | Bioorg Med Chem (2007) 15: 4152-4158 [PMID:17420132] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by 4-NPA hydrolysis assay | B | 5.17 | pKi | 6800 | nM | Ki | J Med Chem (2008) 51: 2518-2521 [PMID:18363349] |
| ChEMBL | Inhibitory effect on human Carbonic anhydrase II | B | 5.37 | pKi | 4300 | nM | Ki | J Med Chem (2002) 45: 312-320 [PMID:11784136] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | B | 5.97 | pKi | 1070 | nM | Ki | Eur J Med Chem (2012) 49: 68-73 [PMID:22245047] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 esterase activity using 4-nitrophenylacetate as substrate | B | 5.97 | pKi | 1070 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1352-1357 [PMID:22230050] |
| ChEMBL | Inhibition of human wild type carbonic anhydrase 2 Asn67Ile mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 6.52 | pKi | 303 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Inhibition of human wild type carbonic anhydrase 2 Gln92Val mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 7.17 | pKi | 68.1 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Mean inhibitory constant towards human carbonic anhydrase II determined by stopped-flow method after 1 hr of incubation | B | 7.45 | pKi | 35.2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2315-2320 [PMID:15837316] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| ChEMBL | Inhibition of human cloned CA2 by CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human cloned CA2 by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| ChEMBL | Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.5 | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841] |
| ChEMBL | Inhibition of human recombinant CA2 cytosolic isoform by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 after 15 mins by CO2 hydrase assay at pH 7.5 | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2011) 19: 1847-1851 [PMID:21377369] |
| ChEMBL | Inhibition of human recombinant alpha-carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3170-3173 [PMID:19435663] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated with compound for 15 mins by carbon dioxide hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant full length CA2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2011) 19: 7003-7007 [PMID:22041171] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
| ChEMBL | Inhibition of human recombinant full length CA2-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| ChEMBL | Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| ChEMBL | Inhibition of human recombinant CA2 | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2006) 49: 5544-5551 [PMID:16942027] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
| ChEMBL | Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3550-3555 [PMID:26174556] |
| ChEMBL | Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| ChEMBL | Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1253-1259 [PMID:26832216] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| ChEMBL | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| ChEMBL | Mean inhibitory constant towards human carbonic anhydrase II determined by stopped-flow method | B | 7.99 | pKi | 10.3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2315-2320 [PMID:15837316] |
| Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7] | ||||||||
| ChEMBL | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 6.01 | pKi | 971 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
| ChEMBL | Inhibition of Cryptococcus neoformans recombinant Can2 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| Carbonic anhydrase 3 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944498] [UniProtKB: Q3SZX4] | ||||||||
| ChEMBL | Inhibition of bovine carbonic anhydrase 3 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | B | 5.07 | pKi | 8510 | nM | Ki | Eur J Med Chem (2012) 49: 68-73 [PMID:22245047] |
| carbonic anhydrase 4/Carbonic anhydrase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 4 esterase activity using 4-nitrophenylacetate as substrate | B | 4.42 | pKi | 38450 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1352-1357 [PMID:22230050] |
| ChEMBL | Inhibition of human carbonic anhydrase 4 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | B | 4.42 | pKi | 38450 | nM | Ki | Eur J Med Chem (2012) 49: 68-73 [PMID:22245047] |
| ChEMBL | Inhibition of truncated human cloned membrane-associated carbonic anhydrase 4 preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 5.07 | pKi | 8590 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human recombinant CA4 by stopped flow CO2 hydrase assay | B | 5.07 | pKi | 8590 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 5A/Carbonic anhydrase 5A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 5A | B | 7.69 | pKd | 20.6 | nM | Kd | Bioorg Med Chem (2007) 15: 4152-4158 [PMID:17420132] |
| ChEMBL | Inhibition of full length human recombinant mitochondrial carbonic anhydrase 5A pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 4.7 | pKi | 20000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human recombinant CA5A by CO2 hydration assay | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of human recombinant full length mitochondrial carbonic anhydrase 5A by stopped-flow CO2 hydration assay | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human recombinant CA5A by stopped flow CO2 hydrase assay | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant CA5A mitochondrial isoform by stopped-flow CO2 hydration assay | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| Carbonic anhydrase 5B, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of full length human recombinant mitochondrial carbonic anhydrase 5B preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 2.22 | pKi | 6033000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human recombinant CA5B by CO2 hydration assay | B | 5.22 | pKi | 6033 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of human recombinant full length mitochondrial carbonic anhydrase 5B by stopped-flow CO2 hydration assay | B | 5.22 | pKi | 6033 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human recombinant CA5B by stopped flow CO2 hydrase assay | B | 5.22 | pKi | 6033 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant CA5B mitochondrial isoform by stopped-flow CO2 hydration assay | B | 5.22 | pKi | 6033 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| Carbonic anhydrase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 6 esterase activity using 4-nitrophenylacetate as substrate | B | 5.62 | pKi | 2420 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1352-1357 [PMID:22230050] |
| ChEMBL | Inhibition of human carbonic anhydrase 6 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | B | 5.62 | pKi | 2420 | nM | Ki | Eur J Med Chem (2012) 49: 68-73 [PMID:22245047] |
| ChEMBL | Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay | B | 7.05 | pKi | 89 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human recombinant CA6 by stopped flow CO2 hydrase assay | B | 7.05 | pKi | 89 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 7/Carbonic anhydrase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| GtoPdb | - | - | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
| ChEMBL | Inhibition of human recombinant CA7 by stopped flow CO2 hydrase assay | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 by stopped flow CO2 hydration method | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3170-3173 [PMID:19435663] |
| ChEMBL | Inhibition of human carbonic anhydrase 7 preincubated with compound for 15 mins by carbon dioxide hydration assay | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant full length CA7-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.93 | pKi | 117 | nM | Ki | Eur J Med Chem (2014) 71: 105-111 [PMID:24287559] |
| ChEMBL | Inhibition of recombinant human CA7 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| carbonic anhydrase 9/Carbonic anhydrase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| ChEMBL | Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibitory constant against catalytic domain of human carbonic anhydrase IX | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human CA9 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem (2011) 19: 7003-7007 [PMID:22041171] |
| ChEMBL | Inhibition of human recombinant CA9 catalytic domain-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2006) 49: 5544-5551 [PMID:16942027] |
| ChEMBL | Inhibition of human cloned CA9 catalytic domain by stopped flow CO2 hydration assay | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6] | ||||||||
| ChEMBL | Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 6.39 | pKi | 411 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| Delta carbonic anhydrase in Thalassiosira weissflogii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097982] [UniProtKB: Q5U9J1] | ||||||||
| ChEMBL | Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.39 | pKi | 404 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
| PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5767] [UniProtKB: P96878] | ||||||||
| ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant Rv3273 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
ChEMBL data shown on this page come from version 36:
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]
