topiramate [Ligand Id: 6849] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL220492 (Epitoma, Epitomax, Eprontia, MCN-4853, Qudexy, Qudexy xr, RWJ-17021, RWJ-17021-000, Sincronil, Topamac, Topamax, Topamax sprinkle, Topimax, Topina, (-)-topiramate, Topiramate, Topiramato, Topomax, Trokendi xr, USL-255, USL255) |
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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 | 4 | pKi | >100000 | 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 | 7.54 | pKi | 29.1 | 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 | 7.54 | pKi | 29.1 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| 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 | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| 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 | 8.18 | pKi | 6.6 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| Carbonic anhydrase 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 | 6.32 | pKi | 474 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
| Carbonic anhydrase in Methanosarcina thermophila (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3932] [UniProtKB: P40881] | ||||||||
| ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila | B | 5.99 | pKi | 1020 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| 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 | 6.44 | pKi | 367 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| Carbonic anhydrase in Methanobacterium thermoautotrophicum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3926] [UniProtKB: Q50565] | ||||||||
| ChEMBL | Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum | B | 4.63 | pKi | 23500 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| 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 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 5.95 | pKi | 1110 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| ChEMBL | Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay | B | 5.96 | pKi | 1108 | 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 | 5.96 | pKi | 1108 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
| 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 | 6.96 | pKi | 110 | 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 | 6.96 | pKi | 110 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| Carbonic anhydrase 1 in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4211] [UniProtKB: O24855] | ||||||||
| ChEMBL | Inhibition of Helicobacter pylori recombinant CA | B | 6.69 | pKi | 205 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| ChEMBL | Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay | B | 6.76 | pKi | 172 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| 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 | 7.11 | pKi | 78 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of mouse recombinant CA15 by stopped flow CO2 hydrase assay | B | 7.11 | pKi | 78 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length mouse carbonic anhydrase 15 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7] | ||||||||
| ChEMBL | Inhibition of Cryptococcus neoformans recombinant Can2 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 6.43 | pKi | 370 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| ChEMBL | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 6.44 | pKi | 367 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
| 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 | 6.11 | pKi | 769 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-9 [PMID:15686894] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 1 assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| ChEMBL | Inhibition of cloned human cytosolic isozyme Carbonic anhydrase I | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2004) 47: 1272-1279 [PMID:14971907] |
| ChEMBL | Inhibitory activity against human cloned carbonic anhydrase I (hCA I) | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 841-845 [PMID:12617904] |
| ChEMBL | Inhibitory effect on human carbonic anhydrase I | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2002) 45: 312-320 [PMID:11784136] |
| ChEMBL | Inhibitory activity against human Carbonic anhydrase I (hCA I) | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2002) 45: 3583-3587 [PMID:12166931] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase I | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2003) 46: 2197-2204 [PMID:12747791] |
| ChEMBL | Ki value against human carbonic anhydrase I | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 971-976 [PMID:15686895] |
| ChEMBL | Ki value against human carbonic anhydrase I (hCA I) | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-969 [PMID:15686894] |
| ChEMBL | Inhibitory activity against human carbonic anhydrase I (hCAI) | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
| ChEMBL | Inhibitory activity against human carbonic anhydrase I at 0.09 uM | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| ChEMBL | Inhibition of human recombinant CA1 | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| ChEMBL | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human recombinant cytosolic isozyme CA I by stopped-flow CO2 hydrase method | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
| ChEMBL | Inhibition of human recombinant CA1 after 15 mins by CO2 hydration stopped flow assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| ChEMBL | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human cloned CA1 by CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of human recombinant full length carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2009) 17: 3659-3664 [PMID:19398204] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human cloned CA1 by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2010) 53: 2913-2926 [PMID:20201556] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 by CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2011) 54: 1481-1489 [PMID:21314129] |
| ChEMBL | Inhibition of human recombinant alpha-carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 1-mediated CO2 hydration activity after 15 mins | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4447-4450 [PMID:21723123] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| ChEMBL | Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay | B | 6.6 | pKi | 250 | 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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2017) 60: 2456-2469 [PMID:28253618] |
| 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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 after 15 mins by stopped flow carbon dioxide hydration assay | B | 6.6 | pKi | 250 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibition of recombinant full length human carbonic anhydrase-1 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | B | 6.6 | pKi | 250 | nM | Ki | Eur J Med Chem (2019) 163: 443-452 [PMID:30530195] |
| ChEMBL | Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
| ChEMBL | Inhibition of recombinant human CA1 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem (2021) 44: 116279-116279 [PMID:34216985] |
| ChEMBL | Compound was evaluated for inhibition against human carbonic anhydrase I | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 217-223 [PMID:14684331] |
| ChEMBL | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| ChEMBL | Inhibitory activity of compound against human carbonic anhydrase I | F | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Binding affinity to human CA2 by ThermoFluor assay | B | 6.54 | pKd | 290 | nM | Kd | J Med Chem (2006) 49: 3496-3500 [PMID:16759092] |
| ChEMBL | Binding affinity to human carbonic anhydrase 2 in presence of 10 mM HEPES and 100 uM Na2SO4 at pH 7.5 by ThermoFluor method | B | 6.54 | pKd | 290 | nM | Kd | J Med Chem (2008) 51: 2518-2521 [PMID:18363349] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 | B | 7.86 | pKd | 13.8 | nM | Kd | Bioorg Med Chem (2007) 15: 4152-4158 [PMID:17420132] |
| ChEMBL | Inhibitory constant value for Carbonic anhydrase II in human determined in pH-shift assay | B | 5.02 | pKi | 9600 | nM | Ki | J Med Chem (2005) 48: 1941-1947 [PMID:15771438] |
| ChEMBL | Inhibitory constant value for Carbonic anhydrase II in human determined in esterase assay | B | 5.11 | pKi | 7700 | nM | Ki | J Med Chem (2005) 48: 1941-1947 [PMID:15771438] |
| ChEMBL | Inhibitory activity against human carbonic anhydrase II at 0.01 uM | B | 5.3 | pKi | 5000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| ChEMBL | Inhibitory constant value for Carbonic anhydrase II in human determined in pH-shift assay | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2005) 48: 1941-1947 [PMID:15771438] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by 4-NPA hydrolysis assay | B | 6.35 | pKi | 450 | nM | Ki | J Med Chem (2008) 51: 2518-2521 [PMID:18363349] |
| ChEMBL | Inhibitory constant value for Carbonic anhydrase II in human determined in esterase assay | B | 6.37 | pKi | 430 | nM | Ki | J Med Chem (2005) 48: 1941-1947 [PMID:15771438] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by CO2 hydration assay | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2013) 56: 9019-9030 [PMID:24205976] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by ThermoFluor method | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2009) 52: 7528-7536 [PMID:19388676] |
| 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 | 6.61 | pKi | 243 | 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 | 7.32 | pKi | 47.8 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (2017) 60: 2456-2469 [PMID:28253618] |
| 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] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 2 assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 after 15 mins by stopped flow carbon dioxide hydration assay | B | 8 | pKi | 10 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibition of recombinant full length human carbonic anhydrase-2 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2019) 163: 443-452 [PMID:30530195] |
| ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
| ChEMBL | Inhibition of recombinant human CA2 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2021) 44: 116279-116279 [PMID:34216985] |
| ChEMBL | Inhibitory activity against human recombinant cytosolic CA2 | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2005) 48: 7860-7866 [PMID:16302824] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
| ChEMBL | Inhibition of human recombinant CA2 | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
| ChEMBL | Inhibition of human cloned CA2 by stopped-flow CO2 hydration method | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human recombinant cytosolic isozyme CA II by stopped-flow CO2 hydrase method | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
| ChEMBL | Inhibition of human recombinant CA2 after 15 mins by CO2 hydration stopped flow assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| ChEMBL | Inhibition of human cloned CA2 by stopped-flow CO2 hydration method | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human cloned CA2 by CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4624-4627 [PMID:18644716] |
| ChEMBL | Inhibition of human recombinant full length carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2009) 17: 3659-3664 [PMID:19398204] |
| ChEMBL | Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow hydration assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human recombinant alpha-carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| ChEMBL | Inhibition of human wild type carbonic anhydrase 2 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
| ChEMBL | Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402] |
| ChEMBL | Inhibitory activity against human carbonic anhydrase II (hCAII) | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
| ChEMBL | Inhibition of cloned human carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2005) 48: 5721-5727 [PMID:16134940] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2010) 53: 2913-2926 [PMID:20201556] |
| ChEMBL | Inhibition of human cytosolic isozyme Carbonic anhydrase II at 20 degree C | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2004) 47: 1272-1279 [PMID:14971907] |
| ChEMBL | Inhibition of human recombinant cytosolic carbonic anhydrase 2-mediated CO2 hydration activity after 15 mins | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4447-4450 [PMID:21723123] |
| ChEMBL | Inhibitory activity against human cloned carbonic anhydrase II (hCA II) | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 841-845 [PMID:12617904] |
| ChEMBL | Inhibitory effect on human Carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2002) 45: 312-320 [PMID:11784136] |
| ChEMBL | Compound was evaluated for inhibition against human carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 217-223 [PMID:14684331] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by CO2 hydration assay | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2011) 54: 1481-1489 [PMID:21314129] |
| ChEMBL | Ki value against human carbonic anhydrase II (hCA II) | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-969 [PMID:15686894] |
| ChEMBL | Inhibition of human cloned CA2 by stopped flow CO2 hydration assay | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2003) 46: 2197-2204 [PMID:12747791] |
| ChEMBL | Inhibitory activity against human Carbonic anhydrase II (hCA II) | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2002) 45: 3583-3587 [PMID:12166931] |
| ChEMBL | Ki value against human carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 971-976 [PMID:15686895] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by CO2 hydration assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2009) 52: 7528-7536 [PMID:19388676] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by CO2 hydration assay | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2013) 56: 9019-9030 [PMID:24205976] |
| ChEMBL | Inhibitory activity of compound against human carbonic anhydrase II | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
| carbonic anhydrase 2/Carbonic anhydrase II in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4706] [GtoPdb: 3092] [UniProtKB: P27139] | ||||||||
| ChEMBL | Inhibition concentration against carbonic anhydrase II in rat determined in esterase assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2005) 48: 1941-1947 [PMID:15771438] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibitory activity against human carbonic anhydrase IV (hCAIV) | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
| ChEMBL | Inhibition of human cloned CA4 by stopped-flow CO2 hydration method | B | 5.31 | pKi | 4900 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human recombinant CA4 after 15 mins by CO2 hydration stopped flow assay | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 4 | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of truncated human cloned membrane-associated carbonic anhydrase 4 preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human cloned CA4 by stopped-flow CO2 hydration method | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant CA4 by stopped flow CO2 hydrase assay | B | 5.31 | pKi | 4900 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 4 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 4 assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 5.31 | pKi | 4900 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| GtoPdb | - | - | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-33 [PMID:16039848] |
| Carbonic anhydrase IV in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL281] [UniProtKB: Q95323] | ||||||||
| ChEMBL | Compound was evaluated for inhibition against bovine carbonic anhydrase IV | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 217-223 [PMID:14684331] |
| ChEMBL | Inhibition of bovine membrane bound isozyme carbonic anhydrase IV isolated from microsomes at 20 degree C | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2004) 47: 1272-1279 [PMID:14971907] |
| ChEMBL | Inhibitory activity against carbonic anhydrase isolated from bovine lung microsome (bCA IV) | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 841-845 [PMID:12617904] |
| ChEMBL | Inhibitory effect on bovine Carbonic anhydrase IV | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2002) 45: 312-320 [PMID:11784136] |
| ChEMBL | Inhibitory activity against bovine carbonic anhydrase IV (bCAIV) | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
| ChEMBL | Inhibitory activity of compound against bovine carbonic anhydrase IV | F | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibitory activity against human carbonic anhydrase IX at 0.09 uM | B | 4.24 | pKi | 58000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
| ChEMBL | Inhibition of human cloned CA9 by stopped-flow CO2 hydration method | B | 5.8 | pKi | 1590 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of full length human recombinant CA IX | B | 5.8 | pKi | 1590 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
| ChEMBL | Inhibitory constant against catalytic domain of human carbonic anhydrase IX | B | 5.8 | pKi | 1590 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| ChEMBL | Inhibition of human recombinant CA9 after 15 mins by CO2 hydration stopped flow assay | B | 5.8 | pKi | 1590 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human cloned CA9 catalytic domain by stopped-flow CO2 hydration method | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydration method | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem (2009) 17: 3659-3664 [PMID:19398204] |
| ChEMBL | Inhibition of human cloned CA9 catalytic domain by stopped flow CO2 hydration assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant CA9 by stopped flow CO2 hydration assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2010) 53: 2913-2926 [PMID:20201556] |
| ChEMBL | Inhibition of human carbonic anhydrase 9 catalytic domain preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human carbonic anhydrase 9 catalytic domain by CO2 hydration assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2011) 54: 1481-1489 [PMID:21314129] |
| ChEMBL | Inhibition of human recombinant transmembrane carbonic anhydrase 9-mediated CO2 hydration activity after 15 mins | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4447-4450 [PMID:21723123] |
| ChEMBL | Inhibition of human recombinant CA9 catalytic domain-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| 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 | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
| ChEMBL | Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| ChEMBL | Inhibition of human carbonic anhydrase 9 after 15 mins by stopped flow carbon dioxide hydration assay | B | 7.24 | pKi | 58 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibition of human carbonic anhydrase-9 catalytic domain assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | B | 7.24 | pKi | 58 | nM | Ki | Eur J Med Chem (2019) 163: 443-452 [PMID:30530195] |
| ChEMBL | Compound was evaluated for inhibition against human carbonic anhydrase IX | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 217-223 [PMID:14684331] |
| ChEMBL | Inhibition of full length human CA9 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem (2021) 44: 116279-116279 [PMID:34216985] |
| ChEMBL | Inhibition of catalytic domain of human recombinant carbonic anhydrase IX | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2005) 48: 5721-5727 [PMID:16134940] |
| ChEMBL | Inhibition of catalytic domain of human cloned CA9 by stopped-flow CO2 hydration method | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of catalytic domain of human recombinant CA IX | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
| ChEMBL | Inhibition of human carbonic anhydrase 9 | B | 7.24 | pKi | 58 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 5A | B | 7.6 | pKd | 25.4 | 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 | 4.2 | pKi | 63000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human cloned CA5A by stopped-flow CO2 hydration method | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human recombinant CA5A after 15 mins by CO2 hydration stopped flow assay | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 5A | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human cloned CA5A by stopped-flow CO2 hydration method | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant CA5A by CO2 hydration assay | B | 7.2 | pKi | 63 | 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 | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human recombinant CA5A by stopped flow CO2 hydrase assay | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 5a preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human recombinant CA5A mitochondrial isoform by stopped-flow CO2 hydration assay | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human carbonic anhydrase 5A after 15 mins by stopped flow carbon dioxide hydration assay | B | 7.2 | pKi | 63 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibitory activity against human recombinant mitochondrial isozyme CA VA | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2005) 48: 7860-7866 [PMID:16302824] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 5A assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| Carbonic anhydrase VB 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 | 4.52 | pKi | 30000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6332-6335 [PMID:18990571] |
| ChEMBL | Inhibition of human cloned CA5B by stopped-flow CO2 hydration method | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human carbonic anhydrase 5B | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human cloned CA5B by stopped-flow CO2 hydration method | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant CA5B by CO2 hydration assay | B | 7.52 | pKi | 30 | 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 | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem (2009) 17: 4894-4899 [PMID:19539481] |
| ChEMBL | Inhibition of human recombinant CA5B by stopped flow CO2 hydrase assay | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 5b preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human recombinant CA5B mitochondrial isoform by stopped-flow CO2 hydration assay | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1334-1337 [PMID:21300547] |
| ChEMBL | Inhibition of human carbonic anhydrase 5B after 15 mins by stopped flow carbon dioxide hydration assay | B | 7.52 | pKi | 30 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibitory activity against human recombinant mitochondrial isozyme CA VB | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2005) 48: 7860-7866 [PMID:16302824] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 5B assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of full length human recombinant CA VI | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
| ChEMBL | Inhibition of human carbonic anhydrase 6 | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
| ChEMBL | Inhibition of human cloned CA6 by stopped-flow CO2 hydration method | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant CA6 by stopped flow CO2 hydrase assay | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human carbonic anhydrase 6 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| ChEMBL | Inhibition of recombinant human CA7 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| ChEMBL | Inhibition of human carbonic anhydrase 7 after 15 mins by stopped flow carbon dioxide hydration assay | B | 8.05 | pKi | 9 | nM | Ki | ACS Med Chem Lett (2018) 9: 462-467 [PMID:29795760] |
| ChEMBL | Inhibition of human recombinant CA7 after 15 mins by CO2 hydration stopped flow assay | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 7 | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human cloned CA7 by stopped-flow CO2 hydration method | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human recombinant CA7 by stopped flow CO2 hydrase assay | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 7 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human recombinant CAH7 | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2011) 54: 2522-2526 [PMID:21395315] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 by stopped flow CO2 hydration method | B | 9.05 | pKi | 0.9 | 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 | 9.05 | pKi | 0.9 | 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 | 9.05 | pKi | 0.9 | 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 | 9.05 | pKi | 0.9 | 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 | 9.05 | pKi | 0.9 | 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 | 9.05 | pKi | 0.9 | nM | Ki | Eur J Med Chem (2014) 71: 105-111 [PMID:24287559] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 7 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2017) 60: 2456-2469 [PMID:28253618] |
| ChEMBL | Inhibition of recombinant full length human carbonic anhydrase-7 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | B | 9.05 | pKi | 0.9 | nM | Ki | Eur J Med Chem (2019) 163: 443-452 [PMID:30530195] |
| ChEMBL | Inhibition of recombinant human CA7 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2021) 44: 116279-116279 [PMID:34216985] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 7 assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| ChEMBL | Inhibition of human cloned CA7 by stopped-flow CO2 hydration method | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| GtoPdb | - | - | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
| ChEMBL | Inhibition of human carbonic anhydrase 7 by CO2 hydration assay | B | 9.06 | pKi | 0.87 | nM | Ki | Eur J Med Chem (2008) 43: 2853-2860 [PMID:18406497] |
| ChEMBL | Ki value against human carbonic anhydrase VII | B | 9.06 | pKi | 0.87 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 971-976 [PMID:15686895] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of recombinant human CA12 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | B | 4.96 | pKi | 11000 | nM | Ki | J Med Chem (2021) 64: 3100-3114 [PMID:33721499] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 by CO2 hydration assay | B | 5.42 | pKi | 3800 | nM | Ki | Eur J Med Chem (2008) 43: 2853-2860 [PMID:18406497] |
| ChEMBL | Inhibitory constant against catalytic domain of human carbonic anhydrase XII | B | 5.42 | pKi | 3800 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| GtoPdb | - | - | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-9 [PMID:15686894] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human cloned CA12 catalytic domain by stopped-flow CO2 hydration method | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human cloned CA12 catalytic domain by stopped flow CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2009) 52: 6421-6432 [PMID:19827837] |
| ChEMBL | Inhibition of human recombinant CA12 by stopped flow CO2 hydrase assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of human recombinant CA12 by stopped flow CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2010) 53: 2913-2926 [PMID:20201556] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 catalytic domain preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 catalytic domain by CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2011) 54: 1481-1489 [PMID:21314129] |
| ChEMBL | Inhibition of human recombinant transmembrane carbonic anhydrase 12-mediated CO2 hydration activity after 15 mins | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4447-4450 [PMID:21723123] |
| 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 | 8.42 | pKi | 3.8 | 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 | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2017) 60: 2456-2469 [PMID:28253618] |
| ChEMBL | Binding affinity to human recombinant carbonic anhydrase 12 assessed as inhibition constant incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2023) 66: 10010-10026 [PMID:37436184] |
| ChEMBL | Ki value against human carbonic anhydrase XII (hCA XII) | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-969 [PMID:15686894] |
| ChEMBL | Inhibition of catalytic domain of human cloned CA12 by stopped-flow CO2 hydration method | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| carbonic anhydrase 13/Carbonic anhydrase XIII 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 | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1] | ||||||||
| ChEMBL | Inhibition of murine CA13 by stopped-flow CO2 hydration method | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of mouse carbonic anhydrase 13 | B | 7.33 | pKi | 47 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of mouse CA13 by stopped-flow CO2 hydration method | B | 7.33 | pKi | 47 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of full length mouse carbonic anhydrase 13 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.33 | pKi | 47 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| carbonic anhydrase 14/Carbonic anhydrase XIV 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 | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3828-3833 [PMID:16039848] |
| ChEMBL | Inhibition of human cloned CA14 by stopped-flow CO2 hydration method | B | 5.84 | pKi | 1460 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
| ChEMBL | Inhibition of human recombinant CA14 after 15 mins by CO2 hydration stopped flow assay | B | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2685-2691 [PMID:17376683] |
| ChEMBL | Inhibition of human carbonic anhydrase 14 | B | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
| ChEMBL | Inhibition of human cloned CA14 by stopped-flow CO2 hydration method | B | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4282-4286 [PMID:18640037] |
| ChEMBL | Inhibition of human carbonic anhydrase 14 by CO2 hydration assay | B | 5.84 | pKi | 1460 | nM | Ki | Eur J Med Chem (2008) 43: 2853-2860 [PMID:18406497] |
| ChEMBL | Inhibition of human recombinant full length carbonic anhydrase 14 by stopped flow CO2 hydration method | B | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem (2009) 17: 3659-3664 [PMID:19398204] |
| ChEMBL | Inhibition of human recombinant CA14 by stopped flow CO2 hydrase assay | B | 5.84 | pKi | 1460 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| ChEMBL | Inhibition of full length human carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 5.84 | pKi | 1460 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3601-3605 [PMID:20472429] |
| ChEMBL | Inhibition of human carbonic anhydrase 14 preincubated with compound for 15 mins by carbon dioxide hydration assay | B | 5.84 | pKi | 1460 | nM | Ki | J Med Chem (2011) 54: 3977-3981 [PMID:21506569] |
| ChEMBL | Inhibition of human recombinant full length CA14-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | B | 5.84 | pKi | 1460 | nM | Ki | J Med Chem (2012) 55: 3891-3899 [PMID:22443141] |
| ChEMBL | Inhibition of human carbonic anhydrase-14 catalytic domain assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | B | 5.84 | pKi | 1460 | nM | Ki | Eur J Med Chem (2019) 163: 443-452 [PMID:30530195] |
| 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 | 6.41 | pKi | 392 | 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 | 5.52 | pKi | 3020 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
| Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775] | ||||||||
| ChEMBL | Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-clamp technique | B | 4.01 | pIC50 | 97000 | nM | IC50 | J Med Chem (2009) 52: 7528-7536 [PMID:19388676] |
| ChEMBL | Inhibition of rat Nav1.2 expressed in CHL1610 cells at -67 to -107 mV after 2 to 3 mins by whole-cell patch-clamp assay | B | 4.01 | pIC50 | 97000 | nM | IC50 | J Med Chem (2013) 56: 9019-9030 [PMID:24205976] |
| Uncharacterized protein Rv1284/MT1322 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 | 6.21 | pKi | 612 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant Rv1284 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | B | 6.21 | pKi | 610 | nM | Ki | J Med Chem (2011) 54: 1682-1692 [PMID:21332115] |
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]
