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, 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 | 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 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 | 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 | 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 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 | 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 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 | 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 | 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 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 | 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 | Inhibitory effect on human Carbonic anhydrase II | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2002) 45: 312-320 [PMID:11784136] |
| 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 | 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] |
| 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 | 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 | 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] |
| 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 | 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 | 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] |
| 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 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 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 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] |
| 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] |
| GtoPdb | - | - | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
| 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] |
| 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] |
| 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 | 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] |
| 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] |
| 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 | 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 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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
